SM253
SM253 is an Hsp90 inhibitor that inhibits Hsp90-dependent protein folding. SM253 blocks chaperone function by binding to the N-middle linker region and the C-terminal M domain, reducing co-chaperone and client protein binding and activation. SM253 induces cancer cell apoptosis, activates caspase 3/7, causes cell cycle arrest and reduces cell proliferation, while decreasing Hsp90 client proteins such as AR, FKBP51, PSA, Cdk4, AKT, ERK, and p23, and reducing Hsp27/Hsp70 expression without inducing heat shock proteins. SM253 causes dose-dependent fibronectin loss in cells expressing LRP1. SM253 can be used for research on colon cancer, pancreatic cancer, and prostate cancer.
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- CAS No.: 1610546-52-5
- Formule: C39H52N6O5S
- Masse moléculaire:716.94
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
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Caspase-3 |
Caspase-7 |
HSP90 |
HSP70 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
5.0 μM
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Cytotoxicity against human HCT-116 colon carcinoma cells assessed as viability reduction by CCK8 assay.
Cytotoxicity against human HCT-116 colon carcinoma cells assessed as viability reduction by CCK8 assay.
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25050163 |
| MIA PaCa-2 | IC50 |
5.5 μM
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Cytotoxicity against human MiaPaCa-2 pancreatic carcinoma cells assessed as viability reduction by CCK8 assay.
Cytotoxicity against human MiaPaCa-2 pancreatic carcinoma cells assessed as viability reduction by CCK8 assay.
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25050163 |
| LNCaP | IC50 |
5.68 μM
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Antiproliferative activity against human LNCaP prostate cancer cells assessed as growth inhibition after 4 days by viable cell count using Trypan blue dye exclusion.
Antiproliferative activity against human LNCaP prostate cancer cells assessed as growth inhibition after 4 days by viable cell count using Trypan blue dye exclusion.
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27526951 |
| 22Rv1 | IC50 |
5.46 μM
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Antiproliferative activity against human 22Rv1 prostate cancer cells assessed as growth inhibition after 4 days by viable cell count using Trypan blue dye exclusion.
Antiproliferative activity against human 22Rv1 prostate cancer cells assessed as growth inhibition after 4 days by viable cell count using Trypan blue dye exclusion.
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27526951 |
| PC-3 | IC50 |
7.31 μM
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Antiproliferative activity against human PC-3 prostate cancer cells assessed as growth inhibition after 4 days by viable cell count using Trypan blue dye exclusion.
Antiproliferative activity against human PC-3 prostate cancer cells assessed as growth inhibition after 4 days by viable cell count using Trypan blue dye exclusion.
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27526951 |
In Vitro
SM253 (5 μM; 2 h) inhibits hsp90-mediated protein folding in rabbit reticulocyte lysate, reducing luciferase activity by 42%[1].
SM253 (5-50 μM; 24 h) reduces HSR proteins by approximately 2-4 fold and depletes hsp27 in HCT-116 cells without inducing a heat shock response[1].
SM253 (2-25 μM; 16 h) induces dose-dependent fibronectin loss in LRP1-expressing MEF-1 cells but not in LRP1-deficient PEA-13 cells[3].
The IC50 values of SM253 in HCT-116 and MiaPaCa-2 cells are 5.0 μM and 5.5 μM, respectively[1].
SM253 (2500-10000 nM; 4 days) inhibits the growth of LNCaP, 22Rv1, and PC-3 prostate cancer cells with an IC50 of approximately 5 µM and reduces the proliferation of PC-3 cells[2].
SM253 (5-10 μM; 48 h) reduces Hsp27/Hsp70 and selected Hsp90 client/co-chaperone proteins in LNCaP, 22Rv1, and PC-3 prostate cancer cells without inducing a heat shock response[2].
SM253 (50 μM; 24 h) induces apoptosis in HCT-116 and MiaPaCa-2 cells[1].
SM253 (24 h) increases caspase 3/7 activity 4-fold in HCT-116 and MiaPaCa-2 cells[1].
SM253 (5-10 μM; 48 h) induces caspase-dependent apoptosis in prostate cancer cell lines, and this cell death is blocked by the pan-caspase inhibitor Z-VAD-fmk (HY-16658B)[2].
SM253 (24 h) arrests HCT-116 and MiaPaCa-2 cells in the G0/G1 phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 and MiaPaCa-2 cells
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Concentration:50 μM
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Incubation Time:24 h
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Result:Induced apoptosis in 75% of cells.
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Cell Line:LNCaP, 22Rv1, and PC-3 human prostate cancer cell lines
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Concentration:2500, 5000, 10000 nM (growth/viability); 5 µM (IC50; CFSE/Ki67); 10 µM (2×IC50; CFSE/Ki67)
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Incubation Time:4 days (growth/viability); 48 h (Ki67)
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Result:Produced dose-dependent inhibition of cell growth in LNCaP, 22Rv1, and PC-3 cells with IC50 ~5 µM.
Reduced the percentage of actively proliferating LNCaP cells significantly in CFSE analysis.
Reduced Ki67 positivity significantly in PC-3 cells.
Did not produce statistically significant Ki67 reduction in LNCaP and 22Rv1 cells.
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Cell Line:LNCaP, 22Rv1, and PC-3 human prostate cancer cell lines
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Concentration:5 and 10 μM
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Incubation Time:48 h
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Result:Displayed concentration-dependent cytotoxicity in prostate cancer cell lines.
Increased cleaved caspase-3 levels compared with vehicle-exposed control cells.
Prevented SM253-induced cell death with Z-VAD-fmk, confirming apoptosis.
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Cell Line:LNCaP, 22Rv1, and PC-3 human prostate cancer cell lines
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Concentration:5 and 10 μM
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Incubation Time:48 h
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Result:Decreased expression of Hsp27 and Hsp70 in LNCaP, 22Rv1, and PC-3 cells.
Reduced AR, FKBP51, PSA, Cdk4, AKT, ERK, FKBP52, and p23 dose-dependently in LNCaP cells.
Reduced Cdk4 and AKT expression and reduced p23 in 22Rv1 cells.
Caused a marked ≥2-fold decrease in HOP expression at 2×IC50 but did not affect FKBP52 in 22Rv1 cells.
Did not inhibit Cdk4 or ERK and reduced p23 in PC-3 cells.
- RNA extraction experimental
- Annexin V plus membrane-impermeant dye apoptosis staining
- Immunoprecipitation
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- Protocol for Cell Cycle
- CCK-8/WST-8 Cell Proliferation Assay
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Ki-67 Immunostaining Proliferation Assay
- Flow cytometric DNA-content cell-cycle staining
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Apoptosis Solutions
- MTT Cell Proliferation Assay
Chemical Information
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CAS No. 1610546-52-5
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Masse moléculaire 716.94
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Formule C39H52N6O5S
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SMILES
C([C@@H]1C(=O)N[C@H](CC2=CSC=N2)C(=O)N[C@H](CC(C)C)C(=O)N(C)[C@@H]([C@H](C)C)C(=O)N[C@@H](CC(C)C)C(=O)N1)(C3=CC=CC=C3)C4=CC=CC=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SM253 Related Classifications
HY-120227 Related Classifications
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