OTX015
OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4. Phase 1. (In Vitro) :Birabresib (OTX-015) (500 nM) exposure induces a strong decrease of BRD2, BRD4 and c-MYC and increase of HEXIM1 proteins, while BRD3 expression is unchanged. c-MYC, BRD2, BRD3, BRD4 and HEXIM1 mRNA levels do correlate however with viability following exposure to Birabresib (OTX-015) . Birabresib (OTX-015) (0.1, 1, 5 μM) treatment induces HIV-1 full-length transcripts and viral outgrowth in resting CD4+ T cells from infected individuals receiving suppressive antiretroviral therapy (ART), while exerting minimal toxicity and effects on T cell activation. Birabresib-mediated activation of HIV-1 involves an increase in CDK9 occupancy and RNAP II C-terminal domain (CTD) phosphorylation. (In Vivo) :In MDA-MB-231 murine xenografts, tumor mass is significantly (p < 0.05) reduced by Birabresib (OTX-015) (50 mg/kg) with respect to vehicle-treated animals. Birabresib (OTX-015) in combination with 2 mg/kg RAD001 shows more effective activity than Birabresib alone.
Product Specifications
CAS Number
202590-98-5
Product Name Alternative
HY-15743 | (?) -OTX015
Purity
>98% (HPLC)
Solubility
DMSO:98 mg/mL (199.19 mM) ; Ethanol:98 mg/mL (199.19 mM) ; Water:<1 mg/mL (<1 mM)
Smiles
O=C (NC1=CC=C (O) C=C1) C[C@H]2C3=NN=C (C) N3C4=C (C (C) =C (C) S4) C (C5=CC=C (Cl) C=C5) =N2
Molecular Formula
C25H22ClN5O2S
Molecular Weight
491.99
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
(S) -2- (4- (4-chlorophenyl) -2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl) -N- (4-hydroxyphenyl) acetamide.
Available Sizes
Frequently Asked Questions
Explore Other Products
Browse additional items from our catalog
NOV (Protein NOV Homolog, NovH, Insulin-like Growth Factor-binding Protein 9, IGF-binding Protein 9, IGFBP-9, IBP-9, Nephroblastoma Overexpressed Gene Protein Homolog, CCN Family Member 3, NOVH, IGFBP9, CCN3) (PE)
