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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- CAS No.: 810659-53-1
- Formule: C24H21N3O6S2
- Masse moléculaire:511.57
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
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Bcl-2 1.3 μM (Ki) |
Bcl-xL >100 μM (Ki) |
Caspase-9 |
Caspase-3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CNE | IC50 |
54.92 μM
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Antiproliferative activity of YC137 against human CNE1 NPC cells assessed as viability reduction after 72 hrs by MTT assay.
Antiproliferative activity of YC137 against human CNE1 NPC cells assessed as viability reduction after 72 hrs by MTT assay.
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22033244 |
| SUNE1 | IC50 |
69.86 μM
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Antiproliferative activity of YC137 against human SUNE1 NPC cells assessed as viability reduction after 72 hrs by MTT assay.
Antiproliferative activity of YC137 against human SUNE1 NPC cells assessed as viability reduction after 72 hrs by MTT assay.
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22033244 |
| K562 | IC50 |
150.33 nM
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Inhibition of viability in human K562 cells by cell viability assay using 1000 cells.
Inhibition of viability in human K562 cells by cell viability assay using 1000 cells.
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33707419 |
| K562 | IC50 |
104 nM
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Inhibition of viability in human Shh-K562 cells by cell viability assay using 1000 cells.
Inhibition of viability in human Shh-K562 cells by cell viability assay using 1000 cells.
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33707419 |
| K562 | IC50 |
53.33 nM
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Inhibition of viability in human K562 cells by cell viability assay using 1000 cells when YC137 is used as adjuvant.
Inhibition of viability in human K562 cells by cell viability assay using 1000 cells when YC137 is used as adjuvant.
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33707419 |
| K562 | IC50 |
52 nM
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Inhibition of viability in human Shh-K562 cells by cell viability assay using 1000 cells when YC137 is used as adjuvant.
Inhibition of viability in human Shh-K562 cells by cell viability assay using 1000 cells when YC137 is used as adjuvant.
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33707419 |
In Vitro
YC137 (25-200 nM; 72 h) inhibits cell viability in chronic myeloid leukemia cells (K562 and Shh-K562)[3].
YC137 (12.5-150 nM; 72 h) combined with 0.5 μM Imatinib (HY-15463) exposure re-sensitizes cells to Imatinib in Shh-expressing chronic myeloid leukemia cells (Shh-K562)[3].
YC137 inhibits K562 and Shh-K562 cell viability, with IC50 values of 150.33 and 104 nM when used alone, and 53.33 and 52 nM when used as an adjuvant[6].
YC137 (0.5 μM; 20 h) induces apoptosis in breast cancer cell lines (MB435B, SUM159, MB435L)[2].
YC137 (0.25 μM; 2-24 h) activates caspase 9 and induces cytochrome c release in MB435B breast cancer cells[2].
YC137 (0.5 μM; 24 h) attenuates apoptosis induction in Trastuzumab (HY-P9907)-pretreated MB435B breast cancer cells[2].
YC137 (0.5 μM; 24 h) induces apoptosis in CD34+ hematopoietic progenitor cells (transfected with Bcl-2 and cultured in the absence of growth factors), increasing apoptosis by approximately 2-fold[2].
YC137 (1 μM; 1 h pretreatment) enhances PAO-induced apoptosis in Bax/Bak double-knockout mouse embryonic fibroblasts (DKO MEFs), indicating that YC137 enhances Bax/Bak-independent cell death[4].
YC137 (0.1 - 0.5 μM; 20 h) does not induce apoptosis in normal primary cells (small intestinal epithelial cells FHs, myoblasts, peripheral blood mononuclear cells PBMCs); and does not induce apoptosis in normal CD34+ cells (co-cultured with MB435B)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HK1 and CNE1 human NPC cell lines
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Concentration:1 μM
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Incubation Time:72 h
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Result:Alone or in combination with Cisplatin significantly sensitized cells to apoptosis.
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Cell Line:HK1 and CNE1 human NPC cell lines
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Concentration:1 μM
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Incubation Time:48 h
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Result:Drastically suppressed BCL-2 protein expression without altering BAX expression.
Chemical Information
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CAS No. 810659-53-1
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Masse moléculaire 511.57
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Formule C24H21N3O6S2
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YC137 Related Classifications
HY-123244 Related Classifications
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