Chemical Structure : YC137
CAS No.:
810659-53-1
YC137
(YC-137)
Catalog No.: PC-25524Not For Human Use, Lab Use Only.
YC137 is a specific small molecule inhibitor of Bcl-2 with Ki of 1.3 uM, with no affinity for Bcl-xL (Ki>100 uM), inhibits the binding of the Bid BH3 peptide to Bcl-2, thus disrupting an interaction essential for the antiapoptotic activity of Bcl-2.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
YC137 is a specific small molecule inhibitor of Bcl-2 with Ki of 1.3 uM, with no affinity for Bcl-xL (Ki>100 uM), inhibits the binding of the Bid BH3 peptide to Bcl-2, thus disrupting an interaction essential for the antiapoptotic activity of Bcl-2.
YC137 induced apoptosis of Bcl-2-transfected cells in a dose-dependent manner.
YC137 induces apoptosis in breast cancer cells that express high levels of Bcl-2 but does not have any effect on normal hematopoietic progenitors, peripheral blood mononuclear cells (PBMCs), small intestine epithelial cells, and myoblasts.
Combination of guanine arabinoside and Bcl-2 inhibitor YC137 overcomes the cytarabine resistance in HL-60 leukemia cell line.
Physicochemical Properties
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M.Wt
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511.57
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Formula
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C24H21N3O6S2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-((4,9-dioxo-4,9-dihydronaphtho[2,3-d]thiazol-2-yl)amino)phenyl (methoxycarbonyl)-L-methioninate
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References
1. Nishi R, et al. Cancer Sci. 2013 Apr;104(4):502-7.
2. Real PJ, et al. Cancer Res. 2004 Nov 1;64(21):7947-53.
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