1. Apoptosis
  2. IAP

SM-164 Hydrochloride 

目录号: HY-15989A
产品使用指南

SM-164 Hydrochloride 是一种可渗透细胞的 Smac 类似物。SM-164 与含有 BIR2 和 BIR3 结构域的 XIAP 蛋白结合,IC50 值为 1.39 nM,SM-164 用作 XIAP 的强效拮抗剂。

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SM-164 Hydrochloride Chemical Structure

SM-164 Hydrochloride Chemical Structure

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Size Price Stock Quantity
10 mM * 1 mL in Water ¥7642 In-stock
5 mg ¥4200 In-stock
10 mg ¥6000 In-stock
50 mg ¥18000 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Description

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

IC50 & Target

IC50: 1.39 nM (XIAP)[1]
Ki: 0.56 nM to (XIAP), 0.31 nM to (cIAP-1), 1.1 nM (cIAP-2)[2]

In Vitro

SM-164 is a non-peptide, cell-permeable, bivalent small-molecule, which mimics Smac protein for targeting XIAP. SM-164 binds to XIAP containing both BIR domains with an IC50 value 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 0.56 nM to XIAP protein containing both BIR2 and BIR3 domains. SM-164 has a Ki value of 0.31 nM to cIAP-1 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

SM-164 is evaluated for its ability to inhibit tumor growth. SM-164 is highly effective in inhibition of tumor growth and capable of achieving tumor regression in the MDA-MB-231 xenograft model. 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 reached 750 mm3 (P<0.02)[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 0.8636 mL 4.3182 mL 8.6365 mL
5 mM 0.1727 mL 0.8636 mL 1.7273 mL
10 mM 0.0864 mL 0.4318 mL 0.8636 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[2]

A set of sensitive and quantitative fluorescence polarization (FP)-based assays are developed to determine the binding affinities of our designed Smac mimetics to XIAP BIR3, XIAP containing both BIR2 and BIR3 domains, cIAP-1 BIR3, cIAP-1 containing both BIR2 and BIR3 domains, and cIAP-2 protein. The FP-based assay for XIAP BIR3 protein is measured. Briefly, 5-carboxyfluorescein is coupled to the lysine side chain of a mutated Smac peptide with the sequence (AbuRPFK-Fam) and this fluorescently tagged peptide (named SM5F) is used as the fluorescent tracer in FP-based binding assay to XIAP BIR3. The Kd value of this fluorescent tracer is determined to be 17.9 nM to XIAP BIR3. In competitive binding experiments, a tested compound is incubated with 30 nM of XIAP BIR3 protein and 5 nM of SM5F in the assay buffer (100 mM potassium phosphate, pH 7.5; 100μg/mL bovine gamma globulin; 0.02 % sodium azide)[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

HCT116 colon cancer cells are treated with SM-164 (1, 10, and 100 nM) alone, TNFα alone, or the combination for 48 h. Cell growth inhibition is determined by a WST assay[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
SCID mice (8-10 per group) bearing MDA-MB-231 xenograft tumors are treated i.v. with 1 and 5 mg/kg of SM-164 or 7.5 mg/kg of Taxotere or vehicle control daily, 5 d/wk for 2 wk. Tumor sizes and animal weights are measured thrice a week[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

1157.88

Formula

C₆₂H₈₅ClN₁₄O₆

SMILES

C[C@H](NC)C(N[C@H]1CCCC[C@](CC[C@H]2C(N[C@@H](C3=CC=CC=C3)C4=CN(CCCCC5=CC=C(CCCCN6N=NC([C@@H](NC([C@@H]7CC[C@@](CCCC[C@@H]8NC([C@@H](NC)C)=O)([H])N7C8=O)=O)C9=CC=CC=C9)=C6)C=C5)N=N4)=O)([H])N2C1=O)=O.Cl

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

H2O: ≥ 106 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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产品名称:
SM-164 Hydrochloride
目录号:
HY-15989A
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