Description: ABT-737 is a novel, potent, selective and orally available BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in enzymatic assays, respectively. It does not inhibit Mcl-1, Bcl-B or Bfl-1 etc. It is currently in Phase 2 clinical trial for cancer treatment.

ABT-737, a B cell lymphoma-2 (Bcl-2) family inhibitor, activates apoptosis in cancer cells. Arsenic trioxide is an apoptosis activator that impairs cancer cell

ABT-737 is a small-molecule BH3 mimetic that exhibits single-agent activity against lymphoma and small-cell lung cancer in preclinical studies. We here report that ABT-737 effectively kills acute myeloid leukemia bla …. BCL-2 proteins are critical for cell survival and are overexpressed in many tumors. ABT-737 is a small-molecule BH3 mimetic that BH3 mimetic ABT-737 induces apoptosis. Sample Page Supplementary MaterialsSupplementary Information 41467_2018_7213_MOESM1_ESM. March 10, 2021 by abt737 ABT-737, a BH3 mimetic, induces glutathione depletion and oxidative stress. Howard AN(1), Bridges KA, Meyn RE, Chandra J. Author information: (1)Department of Pediatrics Research, The University of Texas M D Anderson Cancer Center, Box 853, 1515 Holcombe Blvd, Houston, TX 77030, USA. ABT-737 Cat. No.: A8193 CAS No.: 852808-04-9 Formula: C42H45ClN6O5S2 M.Wt: 813.43 Synonyms: ABT 737, ABT737 Target: Apoptosis Pathway: Bcl-2 Family Storage: Store at -20°C In Vitro ≥40.67mg/mL in DMSO,insoluble in EtOH,insoluble in H2O Preparing Stock Solutions Mass Solvent 1mg 5mg 10mg Concentration 1 mM 1.2294 mL 6.1468 mL 12.2936 mL ABT-737 is a novel and potent pan Bcl-2 inhibitor.

Fig. 1 shows ABT-737 is a small molecule drug that inhibits Bcl-2 and Bcl-xL, two members of the Bcl-2 family of evolutionarily-conserved proteins that share B cl-2 H omology (BH) domains. First developed as a potential cancer chemotherapy, it was subsequently identified as a senolytic (a drug that selectively induces cell death in senescent cells ). BH3 Mimetic ABT-737 is an orally bioavailable, selective small molecule B-cell lymphoma 2 (Bcl-2) Homology 3 (BH3) mimetic, with potential pro-apoptotic and antineoplastic activities. ABT-737 binds to the hydrophobic groove of multiple members of the anti-apoptotic Bcl-2 protein family, including Bcl-2, Bcl-xl and Bcl-w. ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy.

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Jernberg-Wiklund H, Loskog, S I A. ABT-737 blockade of. Bcl-2 family apoptosis inhibitors sensitizes B-cell tumors to CAR-T-cell killing. Cancer Gene Ther. 2013

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Kline et al. Leukemia, 2007;21:1549 Product Datasheets ABT-737 disturbs the binding of B cell lymphoma (Bcl)-2 homologous antagonist killer and Bcl-extra large. ABT-737 induces a BAX/BAK-dependent impairment of maximal O 2 consumption rate in sensitive cells.
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BH3 Mimetic ABT-737 is an orally bioavailable, selective small molecule B-cell lymphoma 2 (Bcl-2) Homology 3 (BH3) mimetic, with potential pro-apoptotic and antineoplastic activities. ABT-737 binds to the hydrophobic groove of multiple members of the anti-apoptotic Bcl … 212 rows ABT-737 is a novel, potent, selective and orally available BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in enzymatic assays, … ABT-737(852808-04-9) Reference standards for Pharmacological research.

ABT-737 exhibits anticancer chemotherapeutic and antithrombotic activities. ABT-737 is currently in clinical trials as one component of a combination therapy in the treatment of various cancers such … ABT-737 is a small-molecule inhibitor of the anti-apoptotic proteins Bcl-2, Bcl-X(L) and Bcl-w, with an affinity two to three orders of magnitude more potent than previously reported compounds.
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RNAi screening uncovers Dhx9 as a modifier of ABT-737 resistance in an Eμ-myc/Bcl-2 mouse model. Mills Jr, Malina A, Lee T, Di Paola D, Larsson O, Miething The contract was highly standardised by means of the AB 04 and ABT 06 agreements, and through the AMA AF administrative provisions.