Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.
 
> SM-164 [957135-43-2]

SM-164 [957135-43-2]

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Référence HY-15989-5mg

Conditionnement : 5mg

Marque : MedChemExpress


Description

SM-164 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[1][2]

cIAP-1

0.31 nM (Ki)

cIAP-2

1.1 nM (Ki)

cIAP

 

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
0.039 μM
Compound: 7, SM-164
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
[PMID: 23062821]
MDA-MB-231 IC50
3.3 nM
Compound: 16, SM-164
Growth inhibition of human MDA-MB-231 cells after 2 to 3 hrs by WST8 assay
Growth inhibition of human MDA-MB-231 cells after 2 to 3 hrs by WST8 assay
[PMID: 21462933]
MDA-MB-231 IC50
6.8 nM
Compound: 6, SM-164
Growth inhibition of human MDA-MB-231 cells after 4 days by WST8 assay
Growth inhibition of human MDA-MB-231 cells after 4 days by WST8 assay
[PMID: 22148838]
SK-OV-3 IC50
16 nM
Compound: 6, SM-164
Growth inhibition of human SKOV3 cells after 4 days by WST8 assay
Growth inhibition of human SKOV3 cells after 4 days by WST8 assay
[PMID: 22148838]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SM-164 Related Antibodies

Solvant et solubilité
In Vitro: 

DMSO : 25 mg/mL (22.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8917 mL 4.4586 mL 8.9173 mL
5 mM 0.1783 mL 0.8917 mL 1.7835 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 0.83 mg/mL (0.74 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 0.83 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Pureté et documentation
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