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SM-164

Catalog No. T12932L CAS 957135-43-2

SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains (IC50: 1.39 nM). It acts as an extremely potent antagonist of XIAP.

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SM-164, CAS 957135-43-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 119.00
2 mg	In stock	$ 173.00
5 mg	In stock	$ 289.00
10 mg	In stock	$ 443.00
25 mg	In stock	$ 718.00
50 mg	In stock	$ 996.00

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Purity: 99.92%

Purity: 97.25%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains (IC50: 1.39 nM). It acts as an extremely potent antagonist of XIAP.
Targets&IC50	CIAP2:1.1 nM (Ki), CIAP1:0.31 nM (Ki)
In vitro	SM-164 binds to XIAP being 300 and 7000-times more potent than its monovalent counterparts and the natural Smac AVPI peptide, respectively. The binding affinities of SM-164 to XIAP, cIAP-1, and cIAP-2 proteins are determined using fluorescence-polarization based assays. 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 minimal toxicity to normal human primary cells at 10,000 nM. SM-164 has a Ki value of 0.56 nM to XIAP protein containing both BIR2 and BIR3 domains. SM-164 has a Ki value of 0.31 nM to a cIAP-1 protein containing both BIR2 and BIR3 domains. SM-164 binds to cIAP-2 BIR3 protein with Ki values of 1.1 nM [1][2].
In vivo	SM-164 is highly effective in the inhibition of tumor growth and capable of achieving tumor regression in the MDA-MB-231 xenograft model. SM-164 (1 mg/kg) treatment fully inhibits tumor growth during the treatment. SM-164 (5 mg/kg) treatment 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 (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 reached 750 mm3 (P<0.02) [2].

Molecular Weight	1121.42
Formula	C62H84N14O6
CAS No.	957135-43-2

Storage

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

Solubility Information

DMSO: 5.2 mg/mL (4.64 mM), Sonification is recommended.

References 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.

Citations

1. Huang F, Liang J, Lin Y, et al.Repurposing of Ibrutinib and Quizartinib as potent inhibitors of necroptosis.Communications Biology.2023, 6(1): 972. 2. Li J, Liu X, Liu Y, et al.Saracatinib inhibits necroptosis and ameliorates psoriatic inflammation by targeting MLKL.Cell Death & Disease.2024, 15(2): 122. 3. Chen D, Chen Y, Feng J, et al.Guanine nucleotide exchange factor RABGEF1 facilitates TNF-induced necroptosis by targeting cIAP1.Biochemical and Biophysical Research Communications.2024: 149669.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Apoptosis Compound Library Cuproptosis Compound Library PPI Inhibitor Library Bioactive Compound Library

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Keywords

SM-164 957135-43-2 Apoptosis IAP SM164 SM 164 inhibit Inhibitor inhibitor

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