SM-122
SM-122 is a Smac mimetic and an IAP inhibitor. SM-122 binds the XIAP BIR3, cIAP‑1 BIR3, and cIAP‑2 BIR3 domains with Ki values of 26 nM, 1.0 nM, and 1.8 nM, respectively. SM‑122 triggers intracellular degradation of cIAP‑1 and cIAP‑2 proteins, relieving IAP-mediated inhibition of caspases. SM-122 inhibits cancer cell growth and induces apoptosis and caspase-dependent cell death in tumor cells. SM-122 can be used for research on cancers such as breast cancer and ovarian cancer.
For research use only. We do not sell to patients.
- CAS No.: 874270-38-9
- Formula: C28H36N4O3
- Molecular Weight:476.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[3]|
cIAP-1 1.0 nM (Ki) |
cIAP-2 1.8 nM (Ki) |
XIAP 26 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
0.41 μM
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Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as growth inhibition by WST-8 assay after 4 days exposure.
Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as growth inhibition by WST-8 assay after 4 days exposure.
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18954041 |
| SK-OV-3 | IC50 |
0.9 μM
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Antiproliferative activity against human SK-OV-3 ovarian cancer cells assessed as growth inhibition by WST-8 assay after 4 days exposure.
Antiproliferative activity against human SK-OV-3 ovarian cancer cells assessed as growth inhibition by WST-8 assay after 4 days exposure.
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18954041 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:30 nM, 100 nM, and 1 µM
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Incubation Time:48 h
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Result:Induced apoptosis in MDA-MB-231 cells, with robust apoptosis at 100 nM.
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Cell Line:MDA-MB-231 cells
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Concentration:10, 100, and 1000 nM
alone or 25 µM Z-DEVD-FMK (HY-12466) -
Incubation Time:48 h
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Result:Killed MDA-MB-231 cells in a dose-dependent manner.
Reduced MDA-MB-231 cell viability in a caspase-3/7-dependent manner.
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Somatic Cell Culture
- CCK-8/WST-8 Cell Proliferation Assay
- Cell Counting-Based Growth Curve Assay
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Protocol for Cell Counting and Cell Density Analysis
- Apoptosis Solutions
- MTT Cell Proliferation Assay
Chemical Information
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CAS No. 874270-38-9
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Molecular Weight 476.61
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Formula C28H36N4O3
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SMILES
O=C([C@H]1N2[C@](CCCC[C@@H](C2=O)NC([C@H](C)NC)=O)([H])CC1)NC(C3=CC=CC=C3)C4=CC=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Miura K, et al. cIAP2 as a therapeutic target in colorectal cancer and other malignancies. Expert opinion on therapeutic targets. 2009 Nov;13(11):1333-45. [Content Brief]
[2]. Sun H, et al. Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP). Journal of medicinal chemistry. 2008 Nov 27;51(22):7169-80. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SM-122 Related Classifications
HY-155294 Related Classifications
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