HSP70-IN-9
HSP70-IN-9 is an Hsp70 inhibitor that induces caspase-3,7 activation with an IC50 of 25.2 μM. HSP70-IN-9 reversibly binds to the allosteric pocket of the N-terminal domain, disrupts the Hsp70-HOP-Hsp90 mega-complex, and inhibits client protein refolding, thereby inducing apoptosis and degradation of Hsp90-Hsp70 tumor client proteins, ultimately inhibiting cancer cell growth. HSP70-IN-9 can be used for research on breast cancer, pancreatic cancer, and acute myeloid leukemia.
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- CAS No.: 1268273-85-3
- Formule: C23H26N6OS
- Masse moléculaire:434.56
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Activité biologique
Description
IC50 & Target
[1]|
caspase-3, 7 25.2 μM (IC50) |
HSP70 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Kasumi 1 | IC50 |
20.8 μM
Compound: 27g
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Cytotoxicity against human Kasumi-1 cells after 72 hrs by alamar blue assay
Cytotoxicity against human Kasumi-1 cells after 72 hrs by alamar blue assay
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[PMID: 24548239] |
| MOLM-13 | IC50 |
25.2 μM
Compound: 27g
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Induction of apoptosis in human MOLM13 cells assessed as caspase 3/7 activation after 16 hrs by fluorescence assay
Induction of apoptosis in human MOLM13 cells assessed as caspase 3/7 activation after 16 hrs by fluorescence assay
|
[PMID: 24548239] |
In Vitro
HSP70-IN-9 (compound 27g) (72 h) inhibits the growth of Kasumi-1 acute myeloid leukemia cells with an IC50 of 20.8 μM[1].
HSP70-IN-9 (16 h) induces caspase-3,7 activation in MOLM-13 acute myeloid leukemia cells with an IC50 of 25.2 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1268273-85-3
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Appearance Solid
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Masse moléculaire 434.56
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Formule C23H26N6OS
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Color White to light yellow
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SMILES
O=C(CN)NC1=CC(SC2=CN=C(N3CCN(CC3)C)N=C2C4=CC=CC=C4)=CC=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Pureté et documentation
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Fiche technique (266 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Taldone T, et al. Heat shock protein 70 inhibitors. 2. 2,5'-thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and 3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70. Journal of medicinal chemistry. 2014 Feb 27;57(4):1208-24. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)