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3-(3,5-Dimethyl-4-isoxazolyl)-5-hydroxy-α-phenyl-benzenemethanol is bromodomain ligand acting as a selective inhibitor of the first bromodomain of BRD4. Potential applications involved decreased lifespan of lung adenocarcinoma cell lines and reduction of cell proliferation in leukemia cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 1429129-68-9. Pack Sizes: 10mg, 50mg. Molecular Formula: C18H17NO3, Molecular Weight: 295.33. US Biological Life Sciences.
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ACBI1
ACBI1 is a potent PROTAC degrader of BAF ATPase subunits SMARCA2 and SMARCA4, also degrades the polybromo-associated BAF (PBAF) complex member PBRM1, with DC50s of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 can induce anti-proliferative effects and apoptosis. Synonyms: ACBI 1; ACBI-1; (2S,4R)-N-(2-(2-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenoxy)ethoxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide. CAS No. 2375564-55-7. Molecular formula: C49H58FN9O7S. Mole weight: 936.12.
ARV-771
ARV-771 is a potent BET bromodomain PROTACĀ® Degrader based on von Hippel-Lindau (VHL) E3 ligase, consisting of a BRD4-binding moiety bound to a VHL ligand via a linker. Synonyms: ARV 771; ARV771; (2S,4R)-1-((S)-2-(tert-butyl)-15-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide; L-Prolinamide, N- [2- [3- [2- [ [2- [ (6S) -4- (4-chlorophenyl) -2, 3, 9-trimethyl-6H-thieno [3, 2-f] [1, 2, 4] triazolo [4, 3-a] [1, 4] diazepin-6-yl] acetyl] amino] ethoxy] propoxy] acetyl] -3-methyl-L-valyl-4-hydroxy-N- [ (1S) -1- [4- (4-methyl-5-thiazolyl) phenyl] ethyl] -, (4R)-; N- ({3-[2- ({[ (6S) -4- (4-Chlorophenyl) -2, 3, 9-trimethyl-6H-thieno[3, 2-f][1, 2, 4]triazolo[4, 3-a][1, 4]diazepin-6-yl]acetyl}amino) ethoxy]propoxy}acetyl) -3-methyl-L-valyl- (4R) -4-hydroxy-N-{ (1S) -1-[4- (4-methyl-1, 3-thiazol-5-yl) phenyl]ethyl}-L-prolinamide. Grades: ≥95%. CAS No. 1949837-12-0. Molecular formula: C49H60ClN9O7S2. Mole weight: 986.64.
AT 1
AT 1 is a highly selective BRD4 protein degrader composed of a BET bromodomain inhibitor (+)-JQ1 conjugated to a von Hippel-Lindau (VHL) ligand. Synonyms: BRD4 degrader AT1; (2S,4R)-1-((R)-2-acetamido-3-((6-(2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamido)hexyl)thio)-3-methylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide. Grades: ≥98%. CAS No. 2098836-45-2. Molecular formula: C48H58ClN9O5S3. Mole weight: 972.68.
AT6
AT6 is a PROTAC AT1 analogue, which is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 with highly selectivity to bromodomain (Brd4). Uses: Scientific research. Group: Signaling pathways. CAS No. 2098836-50-9. Pack Sizes: 1 mg; 5 mg; 10 mg; 25 mg. Product ID: HY-112375.
CPI-268456
CPI-268456 is a ligand of bromodomain-containing protein 4 (BRD4). It binds to BRD4 and inhibits LPS-induced IL-6 secretion in THP-1 cells. Synonyms: 2-[(4S)-8-chloro-6-(4-chlorophenyl)-1-methyl-4H-[1,2]oxazolo[5,4-d][2]benzazepin-4-yl]acetamide. Grades: ≥98%. CAS No. 1380087-86-4. Molecular formula: C20H15Cl2N3O2. Mole weight: 400.3.
FHD-609
FHD-609 is a PROTAC degrader and inhibitor of BRD9 ( Bromodomain-containing protein 9 ). FHD-609 targets to ncBAF , can be used for research of wide range of cancers that contain a mutation in a BAF complex subunit. FHD-609 in combination with Telomelysin or INO5401, may play a role in adrenocortical carcinoma (ACC) treatment. (Blue: BRD9 ligand-6 (HY-49393), Black: linker (HY-168309); Pink: (S)-Deoxy-thalidomide-Br (HY-168308) ) [1] [2] [3] [4] [5]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2676211-64-4. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-153367.
RVX-208
RVX-208 is a potent inhibitor of BET bromodomains. RVX-208 functions by removing atherosclerotic plaque via reverse cholesterol transport (RCT). RVX-208 increases the production of ApoA-I in hepatocytes in vitro, and in vivo in monkeys and humans, which results in increased HDL-C, but the molecular target was not previously reported. Using binding assays and X-ray crystallography, we now show that RVX-208 selectively binds to bromodomains of the BET (Bromodomain and Extra Terminal) family, competing for a site bound by the endogenous ligand, acetylated lysine, and that this accounts for its pharmacological activity. siRNA experiments further suggest that induction of ApoA-I mRNA is mediated by BET family member BRD4. These data indicate that RVX-208 increases ApoA-I production through an epigenetic mechanism and suggests that BET inhibition may be a promising new approach to the treatment of atherosclerosis. Synonyms: RVX208; RVX 208; RVX-208; Apabetalone. Grades: >98%. CAS No. 1044870-39-4. Molecular formula: C20H22N2O5. Mole weight: 370.40.
TC AC 28
TC AC 28 is a high affinity BET bromodomain ligand (Kd = 40 and 800 nM for Brd2(2) and Brd2(1), respectively) with 20-fold selectively for the second over the first bromodomain. Synonyms: TC-AC28, TC AC28, TCAC28; 6-(1H-Indol-4-yl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetic acid methyl ester. Grades: ≥98% by HPLC. CAS No. 1809296-92-1. Molecular formula: C23H21N5O3. Mole weight: 415.44.
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