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Technical Data
| Formula | C62H84N14O6 |
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| Molecular Weight | 1121.42 | CAS No. | 957135-43-2 | |
| Solubility (25°C)* | In vitro | DMSO | 3 mg/mL (2.67 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | SM-164 is a potent, non-peptide, cell-permeable antagonist of XIAP that targets both the BIR2 and BIR3 domains with IC50 of 1.39 nM. SM-164 induces apoptosis and tumor regression. | ||
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| Targets |
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| In vitro | SM-164 binds to XIAP containing both BIR domains with IC50 of 1.39 nM, being 300 and 7000 times more potent than its monovalent counterparts and the natural Smac AVPI peptide, respectively. SM-164 targets cellular XIAP and effectively induces apoptosis at concentrations as low as 1 nM in the HL-60 leukemia cell line. [1] SM-164 induces caspase-8– and caspase-3–dependent apoptosis in cancer cells. SM-164 induces TNFα-dependent apoptosis and cIAP-1 degradation. [2] SM-164 is highly synergistic with TRAIL in vitro in both TRAIL-sensitive and TRAIL-resistant cancer cell lines of breast, prostate, and colon cancer. SM-164 enhances TRAIL-induced apoptosis in cancer cells through amplification of the caspase-8–mediated extrinsic apoptosis pathway [3] |
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| In vivo | SM-164 induces rapid cIAP-1 degradation and strong apoptosis in the MDA-MB-231 xenograft tumor tissues and achieves tumor regression, but has no toxicity in normal mouse tissues. [2] SM-164 induces cIAP1 degradation in tumor tissues and dramatically enhances the in vivoantitumor activity of TRAIL, and the combination of SM-164 and TRAIL achieves tumor regression without toxicity to animals. [3] |
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| Features | The potency of bivalent SM-164 in binding, functional, and cellular assays is 2−3 orders of magnitude higher than its corresponding monovalent Smac mimetics. |
Biological Activity
| Description | SM-164 is a potent, non-peptide, cell-permeable antagonist of XIAP that targets both the BIR2 and BIR3 domains with IC50 of 1.39 nM. SM-164 induces apoptosis and tumor regression. | ||
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| Targets |
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Protocol (from reference)
Selleck's SM-164 has been cited by 16 publications
| CSFV restricts necroptosis to sustain infection by inducing autophagy/mitophagy-targeted degradation of RIPK3 [ Microbiol Spectr, 2024, 12(1):e0275823] | PubMed: 38100396 |
| Intracellular biliverdin dynamics during ferroptosis [ J Biochem, 2024, mvae067] | PubMed: 39340324 |
| Uptake-independent killing of macrophages by extracellular Mycobacterium tuberculosis aggregates [ EMBO J, 2023, 42(9):e113490] | PubMed: 36920246 |
| Uptake-independent killing of macrophages by extracellular Mycobacterium tuberculosis aggregates [ EMBO J, 2023, e113490.] | PubMed: 36920246 |
| TRAF2/3 deficient B cells resist DNA damage-induced apoptosis via NF-κB2/XIAP/cIAP2 axis and IAP antagonist sensitizes mutant lymphomas to chemotherapeutic drugs [ Cell Death Dis, 2023, 14(9):599] | PubMed: 37679334 |
| TRAF2/3 deficient B cells resist DNA damage-induced apoptosis via NF-κB2/XIAP/cIAP2 axis and IAP antagonist sensitizes mutant lymphomas to chemotherapeutic drugs [ Cell Death Dis, 2023, 14(9):599] | PubMed: 37679334 |
| Epithelial Gab1 calibrates RIPK3-dependent necroptosis to prevent intestinal inflammation [ JCI Insight, 2023, 8(6)e162701] | PubMed: 36795486 |
| Mycoplasma hyorhinis infection promotes TNF-α signaling and SMAC mimetic-mediated apoptosis in human prostate cancer [ Heliyon, 2023, 9(10):e20655] | PubMed: 37867861 |
| Mycoplasma hyorhinis infection promotes TNF-α signaling and SMAC mimetic-mediated apoptosis in human prostate cancer [ Heliyon, 2023, 9(10):e20655] | PubMed: 37867861 |
| Salt-inducible kinases inhibitor HG-9-91-01 targets RIPK3 kinase activity to alleviate necroptosis-mediated inflammatory injury [ Cell Death Dis, 2022, 13(2):188] | PubMed: 35217652 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.