Recombinant IL-1β (Peprotech, Cranbury, NJ) was reconstituted RPMI at 0. 12:01PM IST Vir Savarkar (Port Blair) - IXZ. WGK 3. Applications Products Services Documents Support. They are epigenetic readers of histone acetylation with broad specificity. , Suite 700 Toronto, ON, M5G 1L7 Canada +1 416-946-0237. 3; Cell proliferation assay with the AML cell line MV-4−11 that has a MLL-AF4 rearrangement (3 days): growth inhibition with pIC50 = 7. Email: Sales@ChemShuttle. Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). GSK778 has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells, GSK778 reduces the clonogenic capacity of primary human AML cells. rednibar) and I. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Available to order from Sigma-Aldrich. BRD4 inhibitors effectively penetrate the blood-brain barrier and target glioma tumor tissues but have little effect on normal brain tissues. Applications Products Services Documents Support. SML3234. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. 61: Molecular Formula: C 30 H 33 N 5 O 3. GSK778 (68), yielded by introducing an additional pyrrolidine to compound 19 (Fig. 0; BRD4 (BD2) pKd = 5. 1B, fig. 7 B) indicated that GSK778 maintains all of the critical interactions of I-BET151 with BRD4-BD1, including the hydrogen bonding interaction of the 3,5-dimethylisoxazole moiety with the conserved Asn140, the hydrophobic interaction of the aryl ring of the α-methylbenzyl group with the. SML3234. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 Hydrochloride. All Photos (1) Documents. ≥98% (HPLC) All Photos (1)GSK778 (iBET-BD1) est un inhibiteur de bromodomaine BD1 puissant et sélectif des protéines BET, avec des IC50 de 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1) et 143 nM (BRDT BD1) , respectivement. AA Blocks. COO/ COA. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. 11 - Combustible Solids. Copy Link. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Instead, a unique effect of BD2-selective antagonism was revealed with GSK046 affecting the induction of gene expression more so than the expression of steady-state genes, in contrast to GSK778 . GD EN. (a) Phylogenetic tree of bromodomains, with available chemical probes noted; the BET subfamily and the divergence of its first and second bromodomains, BD1 and BD2, are highlighted (adapted from chromohub. GSK778 Hydrochloride. LT EN. ≥98% (HPLC)Herein, GSK778 and GSK046 are referred to as iBET-BD1 and iBET-BD2, respectively. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. GSK778. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. 0. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. nM, SPR BRD4 (BD1): pKd= 8. Binding free energy predictions suggest that entropy changes, electrostatic interactions, and van der Waals interactions are key factors in the selective binding of BD1 and BD2 by SG3-179, GSK778. SML3234. Molecular Formula: C30H33N5O3. Chemical probes developed by the EUbOPEN consortium are peer reviewed by an external committee. Theoretical Analysis Hodoodo Cat#: H408120 Name: GSK778 CAS#: 2451862-42-1By surface plasmon resonance binding assay, GSK778 is > 130-fold selective for BD1, whereas GSK046 is > 300-fold selective for BD2 [26]. GSK778. P (moc. (A) Schematic of the BET Bromodomain proteins and chemical structures. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. , 2020). 8902. 00. Safety Information. a Left panel: MK2206-resistant cell lines were established by growing T47D and ZR75 cells in increasing. Email. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Catalog No. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. Europe PMC is an archive of life sciences journal literature. 14 GSK778, another pan-D1-selective inhibitor (Figure 1A), was recently reported. 11 - Combustible Solids. Federal government websites often end in . Available to order from Sigma-Aldrich. Additionally, while GSK778 phenocopied I-BET151 in terms of anti-proliferative effects on a range of human cancer cells, GSK046 was less effective. 451491-47-7 CTB (Cholera Toxin B subunit) is an activator of p300 histone acetyltransferase and induces apoptosis in MCF-7 cells. Copy Link. But, how does GSK778 work on the target? Let’s discuss it in detail. BET proteins are linked to cancer progression. Applications Products Services Documents Support. Email. R (moc. S1F. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. SA EN. But, how does GSK778 work on the target? Let’s discuss it in detail. $21. All Photos (1) Documents. The. GSK778. SML3168. Probe criteria. WGK. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Molecular Formula: C30H33N5O3. $79. Applications Products Services Documents Support. At. G-Protein-coupled Receptor Ligands. GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75. 6swo: c-terminal bromodomain of human brd2 with ibet-bd1 (gsk778)BRD3. Available to order from Sigma-Aldrich. GSK778 Hydrochloride. , 2020; Gilan et al. These challenging conclusions were drawn based on the similarity of antitumor effects as well as the gene expression spectrums between BD1-selective compound iBET-BD1 (GSK778) and the pan-BET inhibitor iBET-151 (Gilan et al. GSK778 : Catalog Number: M10828: CAS Number: 2451862-42-1: 1. 1B, fig. Given the high sequence similarity amongst BET bromodomains, small molecule inhibitors for a single BET bromodomain are lacking; however, potent pan-D2 inhibitors (e. ZA EN. Copy Link. BD1 selective inhibitors, such as GSK778, MS-436, Olinone, and BI-2536, as well as the BD2 selective inhibitors RVX-208, RVX-297, GSK046, and ABBV-744 have been produced. 0; BRD4 (BD2) pKd = 5. ksg@ajoir. CAS: 2451862-42-1 (free base) Chemical Name: GSK778 2HCl; 4-(2-(Methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H. In contrast to other reported domain-selective molecules, these compounds showed little binding to bromodomains outside of. SML3234. 65 In turn, pan-BD2 inhibitors (which have higher inhibitory activity for BD2 than BD1 of BET family members) are. GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75 nM for BRD2 BD1, 41 nM for BRD3 BD1, 41 nM for BRD4 BD1, and 143 nM for BRDT BD1. Email. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. selective (GSK778) or BD2-selective (GSK046 and ABBV-744) BETis showed signicant IC 50 value dierences between BD1 and BD2 2,9,22,23. Find (s)-1-phenylethyl (r)-acetoxyphenylacetate and related products for scientific research at MilliporeSigmaI-BET151 (GSK1210151A), iBET-BD1 (GSK778) and iBET-BD2 (GSK046) were provided by GlaxoSmithKline plc (GSK, London, UK). Phone: +1 510. BD1 selective inhibitors, such as GSK778, MS-436, Olinone, and BI-2536, as well as the BD2 selective inhibitors RVX-208, RVX-297, GSK046, and ABBV-744 have been produced. 4 D and E) shows that our BD1-selective and BD2-selective DECL-derived inhibitors each occupy the same KAc pocket as GSK778 but also access adjacent grooves that differ between the two domain types. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. They are epigenetic readers of histone acetylation with broad specificity. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. A concentration of 1-2 µM of I-BET151, GSK778, GSK789, or GSK046 was used for cell culture treatments as recommended by our collaborators at GlaxoSmithKline (54–56). Dagrocorat. SML3234. Pharmacological inhibition of BET BDs using the chemical probes JQ1 (Filippakopoulos et al. 2h 04m. 4. ABBV-744 is highly selective for BD2 of BRD2, BRD3 and BRD4, 64 exhibiting several hundred-fold higher affinity for the BD2 over BD1. GSK778 hydrochloride hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Selectivity profile of I-BET151, iBET-BD1 (GSK778) and iBET-BD2 (GSK046). All Photos (1) Documents. ≥98% (HPLC) All Photos (1)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 3 Details of the supplier of the safety data sheet; Company: Abmole Bioscience Inc. Available to order from Sigma-Aldrich. Applications Products Services Documents Support. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. The second-generation BRD4 inhibitors are mainly synthesized by proteolysis targeting chimera (PROTAC) technology. Membranes were blocked with 5% milk in Tris-buffered saline (TBS) with 0. Email. PM EN. 1B, fig. Of these, only ABBV-744 and two molecules described within the article, GSK778 (iBET-BD1) and GSK046 (iBET-BD2) showed appreciable selectivity. GSK778 phenocopies the effects of pan- BET inhibitors in cancer models. This approach Product Description. 6SWN, 6SWO, 6SWP, 6SWQ. Email. Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months). The authors found that in mouse models of various cancers, BD1 inhibition is reminiscent of pan-BET inhibi-tion. Nevertheless, it was more efficacious in a broad range of cancers and inflammatory pathologies [25]. 4. GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). GSK778 Hydrochloride. 1B, fig. RU EN. GSK778. 7 GSK046 (BD2) pIC50 = 7. Your information is safe with us. COO/ COA. 33DFTG (TD139) $21. All Photos (1) Documents. T9703 CAS 2451862-42-1. thesgc. No; GlaxoSmithKline The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer-related and immunity-associated genes. Available to order from Sigma-Aldrich. SML3234. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. COO/ COA. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. The subsequent development and application of GSK778 (BD1 selective) and GSK046 (BD2 selective) revealed that inhibition of BD2 was ineffective in displacing BET proteins from chromatin. All Photos (1) Documents. ≥98% (HPLC)GSK778 ( iBET-BD1 ) Catalog No. Its mechanism of action is not fully understood. 10 µM; GSK791. BET BD1 related products. 11 - Combustible Solids. Copy Link. showed that BD(1)-specific GSK778 phenocopied the effects of pan-BET BRD inhibitors, while GSK046 and its orally bioavailable GSK620 derivative had minimal impact on cell viability while impairing the induction, but not the maintenance, of transcriptional programs [133]. 9. Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. GSK778 (iBET-BD1) ist ein potenter und selektiver BD1-BromodomÄnen-Inhibitor der BET-Proteine mit IC50-Werten von 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1) und 143 nM (BRDT BD1) , beziehungsweise. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778 Hydrochloride. ≥98% (HPLC)Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. Europe PMC is an archive of life sciences journal literature. Instead, a unique effect of BD2-selective antagonism was revealed with GSK046, affecting the induction of gene expression more so than the expression of steady-state genes, in contrast to. COO/ COA. Available to order from Sigma-Aldrich. COO/ COA. The addition of olinone to oligodendrocyte progenitor cells demonstrated biological effects divergent from pan-BET inhibition. Available to order from Sigma-Aldrich. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. iBET-BD1 showed a selectivity of ≥130-fold for BRD4 BD1, and iBET-BD2. ( A ) Schematic of the BET bromodomain proteins and chemical structures. The BD2 selective inhibitor RVX-208 could significantly decrease atherosclerosis in hyperlipidemic apolipoprotein E-deficient mice 14 , and increase high-density lipoprotein cholesterol as well as apolipoprotein A-1 in monkeys 15 . GSK778 Hydrochloride. By Louis Gilman. Le GSK778 montre également de forts effets anti-cancéreux in vivo, prolongeant la survie de souris atteintes de leucémies myéloïdes aiguë [422, 423]. All Photos (1) Documents. BROMODOMAIN AND EXTRA‐TERMINAL (BET) PROTEINS. 5), is a highly selective BD1 inhibitor (BRD4(1), IC 50 = 41 nM) with a 143-fold selectivity over BD2. Applications Products Services Documents Support. As epigenetic readers, bromodomain and extra-terminal domain (BET) family proteins bind to acetylated-lysine residues in histones and recruit protein complexes to promote transcription initiation and elongation. e. Available to order from Sigma-Aldrich. 5% gels (100 V, 90 min) and transferred to nitrocellulose membranes (90 V, 90 min). Developing BDII selective compounds was far more challenging, and only a handful of BDII selective inhibitors have been developed to date (Figure 1). The imidazoquinolinone 8-position of iBET151 was identified as orienting towards the. Applications Products Services Documents Support. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. SML3234. MM EN. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. All Photos (1) Documents. Inhibitor/agonist potency: goal is < 50 nM (IC 50, K D) Surpasses criterion: :BET mutant TR-FRET assay: BRD2 (BD1) pIC 50 = 7. Contains a pharmaceutically active ingredient. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. Solubility: Soluble in DMSO. Herein,. GSK778 Hydrochloride. Copy Link. All Photos (1) Documents. CAS#: 2451862-42-1. Developing BDII selective compounds was far more challenging, and only a handful of BDII selective inhibitors have been developed to date (Figure 1). ID EN. In human whole blood and MV-4–11 cells, selective inhibition of GSK778 against BD1 retains the anti-inflammatory and antiproliferative phenotype features of pan-BET inhibition. 1 in RR-multiple myeloma CC-94280 HIGHLIGHTS FROM DRUG DISCOVERY ARTICLES PUBLISHED ONLINE | MAR. The structures of the two predominant metabolites (M4 and M5) of RVX-208, observed both in in vitro human and animal liver microsomal incubations, as well as in plasma from animal in vivo studies, were determined. Available to order from Sigma-Aldrich. Apart from BRDs, YEATS family members have been. Copy Link. 1A). ChemicalBook 致力于为化学行业用户提供FREEBASE的性质、化学式、分子式、比重、密度,同时也包括FREEBASE的沸点、熔点、MSDS、用途、作用、毒性、价格、生产厂家、用途、上游原料、下游产品等信息。GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. GSK778 Hydrochloride. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. Lymphoma Non. Applications Products Services Documents Support. GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. Available to order from Sigma-Aldrich. COO/ COA. COO/ COA. SML3234. GSK778 Hydrochloride. Copy Link. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Miransertib is a highly selective, orally active, pan-Akt inhibitor. 3. 65 ABBV-744 shows potent anti-proliferative effects against. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. Open in a separate window. Louis Gilman November 13, 2023. 1 Selectivity profile of I-BET151, iBET-BD1 (GSK778), and iBET-BD2 (GSK046). Instead, a unique effect of BD2-selective antagonism was revealed with GSK046 affecting the induction of gene expression more so than the expression of steady-state genes, in contrast to GSK778 . All Photos (1) Documents. Available to order from Sigma-Aldrich. COO/ COA. Chronic Lymphocytic Leukemia Lymphoma Mantle Cell Lymphoma Ibrutinib is a Btk Inhibitor for Autoimmune Disease and B-cell Malignancy Research. Available to order from Sigma-Aldrich. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Fax: +1 510. The distinct families are. GSK778 hydrochloride hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Copy Link. 1 Among these, bromodomain and extraterminal (BET) proteins constitute a unique group with four family members, bromodomain-containing protein 4 (BRD4), BRD3, BRD2, and. • GSK778 exhibits >130-fold BD1 selectivity over BD2 due to BD1 Asp144/His433 displacement (Kharenko et al. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. I-BET151, GSK778, GSK046 and GSK620 are available from R. ChemScene Provide GSK778(CAS 2451862-42-1)In-stock or Backordered impurities,Bulk custom synthesis,Formular C30H33N5O3,MW 511. Solubility: Soluble in DMSO. The bromodomain (BD) is a ~110 amino acid motif that binds to acetyl-lysine modifications on histone and non-histone proteins (Dhalluin et al. Email. 26 (n= 10); 40-fold. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Well-characterized small molecules are essential tools for studying the biology and therapeutic relevance of a target protein. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778에 대한 모든 정보는 Chemicalbook 에서 조회 할 수 있습니다. You can also browse global suppliers,vendor,prices,Price,manufacturers of GSK778(2451862-42-1). GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. $79. 125 nM (MV-4−11 cells) ≤. Herein, GSK778 and GSK046 are referred to as iBET-BD1 and iBET-BD2, respectively. SML3234. GSK778: CAS Registry Number: 2451862-42-1: Molecular Weight: 511. BRD4. IC₅₀ & Target BRD2 BD1 75 nM (IC50) BRD3 BD1 41 nM. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 Hydrochloride. Available to order from Sigma-Aldrich. Recently, BET proteins inhibitors that selectively target BD1 (GSK778, MS-436, Olinone, and BI-2536) and BET proteins inhibitors that selectively target BD2 (GSK046, RVX-208, RVX-297, ABBV-744) have been developed [42-47]. All Photos (1) SML3234. SignificanceBET bromodomain inhibition is therapeutic in multiple diseases; however, pan-BET inhibitors have induced significant myelosuppression and gastrointestinal toxicity, perhaps due to inhib. Safety Information. GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. amni) under a material transfer agreement with GSK. Not for human use. Phylogenetic tree of the human bromodomain-containing protein subgroups. Synonym(s): 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5-dimethylisoxazole Hydrochloride, iBET-BD1. GSK778 (iBET-BD1) potently inhibits numerous cancer cells. All Photos (1) Documents. Safety Information. 2h 41m. E-newsletter Get updates ,discounts and special offers. Copy Link. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Description: GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). CAS: 2451862-42-1 (free base) Chemical Name: GSK778 2HCl; 4-(2-(Methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 reduces the production of anti-keyhole limpet. Available to order from Sigma-Aldrich. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. Catalog Number: AA01KEG7. P. It achieves this complex task by recruiting BRD4, via a pan-BET ligand (JQ1), to the GAA repeats by using a sequence-selective DNA-binding polyamide. ChemicalBook 致力于为化学行业用户提供FREEBASE的性质、化学式、分子式、比重、密度,同时也包括FREEBASE的沸点、熔点、MSDS、用途、作用、毒性、价格、生产厂家、用途、上游原料、下游产品等信息。 Recently, Gilan et al. Potency in Cells and Cellular Target Engagement: GSK778 engages the target in HEK293 cells: pIC50 = 7. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 (iBET-BD1) is a potent and selective inhibitor of the BD1 bromine domain of the BET protein,IC50 The values are 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4. Selectivity profile of I-BET151, iBET-BD1 (GSK778), and iBET-BD2 (GSK046). Drug Formulation: This drug may be formulated in DMSO. Safety Information. SML3234. GM6001. 1. On the basis of sequence homology, BCPs are classified into eight different subgroups (families). Applications Products Services Documents Support. Available to order from Sigma-Aldrich. WGK 3. MedChemExpress provides thousands of inhibitors, modulators and agonists with high purity and quality, excellent customer reviews, precise and professional product citations, tech support and prompt delivery. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Email. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Available to order from Sigma-Aldrich. Their affinities for the individual bromodomains of the BET family were initially determined by TR-FRET (Fig. Storage Class Code. If not otherwise indicated, cells were pretreated with I-BET151, iBET-BD1, iBET-BD2 or vehicle (DMSO) for 48 hours, irradiated with 0 or 6 Gy, and incubated for additional time intervals with concurrent drug. We would like to show you a description here but the site won’t allow us. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. 3; Cell. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Join. The two novel ‘iBET’ molecules display the. GSK778 reduces the production of anti-keyhole limpet. , 2013). S1F, and table S1). 5 (LPS-PBMC assay) <10: 8 GSK620 (BD2) pIC50 = 7. GSK778 reduces the production of anti-keyhole limpet. GSK778 phenocopies the. MH EN. Miransertib target all three Akt isoforms by blocking…. They are useful assets for example, in phenotypic assays, or as a starting point for medicinal chemistry campaigns. To explore the individual functional contributions of BD1 and BD2 in biology and therapy, selective BD1 and BD2 inhibitors have been developed: GSK778 and GSK046 (termed iBET-BD1 and iBET-BD2, respectively) . Domain-Selective Targeting (BD1 or BD2 Targeting) The BET protein family of BCPs comprise the ubiquitously expressed BRD2, BRD3, and BRD4 and the testis-restricted BRDT, all of which harbor two highly conserved tandem bromodomains, BD1 and BD2,.