810659-53-1
Chemical Structure
YC137
- CAS No.: 810659-53-1
- Formula:C24H21N3O6S2
- Molecular Weight:511.57
IUPAC Name: 4-((4,9-dioxo-4,9-dihydronaphtho[2,3-d]thiazol-2-yl)amino)phenyl (methoxycarbonyl)-L-methioninate
InChIKey: SFDSXIZFOOBDMC-KRWDZBQOSA-N
SMILES: CSCC[C@@H](C(OC1=CC=C(NC2=NC(C3=O)=C(C(C4=C3C=CC=C4)=O)S2)C=C1)=O)NC(OC)=O
Biological Activity: YC137 is a potent and selective Bcl-2 inhibitor with a Ki of 1.3 μM. YC137 binds to the BH3-binding groove of the Bcl-2 protein to block its interaction with pro-apoptotic proteins such as Bid and inhibits Bcl-2 expression, thereby triggering mitochondrial depolarization and cytochrome c release, and ultimately activating intrinsic apoptosis mediated by caspase-9 and caspase-3. YC137 can be used for research on nasopharyngeal carcinoma, breast cancer, and chronic myeloid leukemia[1][2][3][4][5][6].
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YC137 | YC137 is a potent and selective Bcl-2 inhibitor with a Ki of 1.3 μM. YC137 binds to the BH3-binding groove of the Bcl-2 protein to block its interaction with pro-apoptotic proteins such as Bid and inhibits Bcl-2 expression, thereby triggering mitochondrial depolarization and cytochrome c release, and ultimately activating intrinsic apoptosis mediated by caspase-9 and caspase-3. YC137 can be used for research on nasopharyngeal carcinoma, breast cancer, and chronic myeloid leukemia. | |||||||||||||||||||||
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References
- [1]. Low SY, et al. Suppression of BCL-2 synergizes cisplatin sensitivity in nasopharyngeal carcinoma cells. Cancer letters. 2012 Jan 28;314(2):166-75.
- [2]. Real PJ, et al. Breast cancer cells can evade apoptosis-mediated selective killing by a novel small molecule inhibitor of Bcl-2. Cancer research. 2004 Nov 1;64(21):7947-53. [Content Brief]
- [3]. Anusha, et al. Exovesicular-Shh confers Imatinib resistance by upregulating Bcl2 expression in chronic myeloid leukemia with variant chromosomes. Cell death & disease. 2021 Mar 11;12(3):259.
- [4]. Ni B, et al. Phenylarsine oxide induces apoptosis in Bax- and Bak-deficient cells through upregulation of Bim. Clinical cancer research : an official journal of the American Association for Cancer Research. 2012 Jan 01;18(1):140-51.
- [5]. Zeitlin BD, et al. Antiangiogenic effect of TW37, a small-molecule inhibitor of Bcl-2. Cancer research. 2006 Sep 01;66(17):8698-706. [Content Brief]
- [6]. Anusha, et al. Exovesicular-Shh confers Imatinib resistance by upregulating Bcl2 expression in chronic myeloid leukemia with variant chromosomes. Cell Death Dis. 2021 Mar 11;12(3):259.
