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SM-164 Hydrochloride (957135-43-2 free base)

Catalog No. T12932   CAS T12932
Synonyms: SM-164 Hydrochloride

SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains(IC50 value of 1.39 nM) and functions as an extremely potent antagonist of XIAP.

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SM-164 Hydrochloride (957135-43-2 free base) Chemical Structure
SM-164 Hydrochloride (957135-43-2 free base), CAS T12932
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5 mg Inquiry $ 372.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains(IC50 value of 1.39 nM) and functions as an extremely potent antagonist of XIAP.
Targets&IC50 XIAP:0.56 nM (ki), XIAP:1.39 nM, cIAP:, cIAP-2:1.1 nM (ki), cIAP-1:0.31 nM (ki)
In vitro SM-164 is a non-peptide, bivalent small-molecule, cell-permeable, which mimics Smac protein for targeting XIAP. SM-164 binds to XIAP containing both BIR domains(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 concurrently interacts with both BIR domains in XIAP and functions as an ultra-potent antagonist of XIAP in both cell-free functional and cell-based assays. SM-164 targets cellular XIAP and effectively induces apoptosis at concentrations as low as 1 nM in leukemia cancer cells, while having a minimal toxicity to normal human primary cells at 10,000 nM[1]. The binding affinities of SM-164 to XIAP, cIAP-1, and cIAP-2 proteins are determined using fluorescence-polarization based assays. SM-164 has a Ki value of 0.31 nM to cIAP-1 protein containing both BIR2 and BIR3 domains.SM-164 has a Ki value of 0.56 nM to XIAP protein containing both BIR2 and BIR3 domains. SM-164 binds to cIAP-2 BIR3 protein with Ki values of 1.1 nM. Addition of exogenous TNFα can significantly enhance the activity of these Smac mimetics, especially for SM-164, in resistant cancer cell lines such as HCT116 and MDA-MB-453[2].
In vivo In the MDA-MB-231 xenograft model ,SM-164 is highly effective in inhibition of tumor growth and capable of achieving tumor regression . Treatment with SM-164 at 1 mg/kg completely inhibits tumor growth during the treatment. Treatment with SM-164 at 5 mg/kg reduces the tumor volume from 147±54 mm3 at the beginning of the treatment (day 25) to 54±32 mm3 at the end of the treatment (day 36), a reduction of 65%. The strong antitumor activity by SM-164 is long lasting and not transient. SM-164 at 5 mg/kg is statistically more effective than Taxotere at the end of the treatment (P<0.01) or when the tumor size in the control group reaches 750 mm3 (P<0.02)[2].
Synonyms SM-164 Hydrochloride
Molecular Weight 1157.88
Formula C62H85ClN14O6
CAS No. T12932

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 106 mg/mL (91.55 mM)

TargetMolReferences and Literature

1. Sun H, et al. Design, synthesis, and characterization of a potent, nonpeptide, cell-permeable, bivalent Smac mimetic that concurrently targets both the BIR2 and BIR3 domains in XIAP. J Am Chem Soc. 2007 Dec 12;129(49):15279-94. 2. Lu J, et al. SM-164: a novel, bivalent Smac mimetic that induces apoptosis and tumor regression by concurrent removal of the blockade of cIAP-1/2 and XIAP. Cancer Res. 2008 Nov 15;68(22):9384-93.

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Keywords

SM-164 Hydrochloride (957135-43-2 free base) T12932 Apoptosis IAP SM164 Hydrochloride SM164 Hydrochloride (957135432 free base) SM 164 Hydrochloride (957135 43 2 free base) 957135-43-2 957135-43-2 free base SM-164 Hydrochloride SM 164 Hydrochloride inhibitor inhibit

 

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