SM-164 [957135-43-2]
Katalog-Nummer HY-15989-10mg
Size : 10mg
Marke : MedChemExpress
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.
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SM-164 Chemische Struktur
CAS. Nr. : 957135-43-2
Größe | Preis | Verfügbarkeit | Menge |
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5 mg | USD 350 | Auf Lager | |
10 mg | USD 600 | Auf Lager | |
50 mg | USD 1800 | Auf Lager | |
100 mg | USD 2520 | Auf Lager | |
200 mg | Angebot einholen | ||
500 mg | Angebot einholen |
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This product is a controlled substance and not for sale in your territory.
Based on 31 publication(s) in Google Scholar
Other Forms of SM-164:
- SM-164 Hydrochloride In-stock
- •Cell Res. 2023 Sep 19. [Abstract]
- •Signal Transduct Target Ther. 2020 Oct 9;5(1):235. [Abstract]
- •Proc Natl Acad Sci U S A. 2022 Sep 6;119(36):e2117396119. [Abstract]
- •Int J Biol Macromol. 2023 Jun 13;125373. [Abstract]
- •Cell Death Dis. 2018 Nov 15;9(12):1140. [Abstract]
- •Cell Death Discov. 2024 Mar 23;10(1):152. [Abstract]
- •Eur J Med Chem. 2024 Mar 9, 116304.
- •J Med Chem. 2023 Mar 12. [Abstract]
- •J Med Chem. 2023 Feb 23;66(4):3073-3087. [Abstract]
- •J Med Chem. 2022 Oct 26. [Abstract]
- •Eur J Med Chem. 2022 Jun 5;236:114345. [Abstract]
- •Mater Sci Eng C Mater Biol Appl. 29 December 2021, 112615.
- •Eur J Med Chem. 2021 Apr 27;220:113484. [Abstract]
- •J Ethnopharmacol. 2023 Nov 1:117373. [Abstract]
- •Bioorg Chem. 2024 Jan, 142, 106964.
- •J Cell Mol Med. 2023 Aug 29. [Abstract]
- •Bioorg Chem. 2023 Jun 1;137:106647. [Abstract]
- •Mol Neurobiol. 2023 Jan 5. [Abstract]
- •Bioorg Chem. 2022: 106339.
- •Rheumatology. 2022 Oct 29;keac621. [Abstract]
- •Bioorg Med Chem. 2024 Mar 1:102:117659. [Abstract]
- •Bioorg Med Chem. 2024 Feb 15:100:117611. [Abstract]
- •Bioorg Med Chem. 2023 Aug 15, 91, 117385.
- •bioRxiv. 2023 Aug 24.
- •Patent. US20230192662A1.
- •bioRxiv. 2023 Apr 25.
- •Research Square Print. 2022 May.
- •Curr Protoc. 2021 Jun;1(6):e156. [Abstract]
- •Biomed Res Int. 2019 Apr 7;2019:2121357. [Abstract]
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SM-164 purchased from MedChemExpress. Usage Cited in: Biomed Res Int. 2019 Apr 7;2019:2121357. [Abstract]
- The mouse alveolar epithelium cell line MLE12 is exposed to SM-164 for 24h with or without LPS for 24h. RIPK3 and MLKL are downregulated along with the inhibition of cIAP2 by SM-164 during LPS-induced ARDS.
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SM-164 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Nov 15;9(12):1140. [Abstract]
- MEF cells are transfected with indicated siRNA for 3 days and then treated with TNF+Smac+zVAD, or poly I:C+zVAD for 3 h.
•Related Screening Libraries:
•Related Small Molecules:
•Related Proteins:
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Beschreibung | |||||||||||||
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IC50 & Target[1][2] |
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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. |
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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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Molekulargewicht |
1121.42 |
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Formel |
C62H84N14O6 |
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CAS. Nr. | |||||||||||||
Appearance |
Solid |
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Color |
White to light yellow |
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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)(21)N7C8=O)=O)C9=CC=CC=C9)=C6)C=C5)N=N4)=O)(21)N2C1=O)=O |
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Versand | Room temperature in continental US; may vary elsewhere. |
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Speicherung |
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Lösungsmittel & Löslichkeit |
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
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
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%
+
%
Tween-80
+
%
Saline
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Reinheit & Dokumentation |
Purity: 99.65% |
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Verweise |
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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.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 0.8917 mL | 4.4586 mL | 8.9173 mL | 22.2932 mL |
5 mM | 0.1783 mL | 0.8917 mL | 1.7835 mL | 4.4586 mL | |
10 mM | 0.0892 mL | 0.4459 mL | 0.8917 mL | 2.2293 mL | |
15 mM | 0.0594 mL | 0.2972 mL | 0.5945 mL | 1.4862 mL | |
20 mM | 0.0446 mL | 0.2229 mL | 0.4459 mL | 1.1147 mL |
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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Massenanfrage
Inquiry Information
- Produktname:
- SM-164
- Art. -Nr.:
- HY-15989
- Menge:
- MCE Japan Authorized Agent: