SIRT2-IN-20
SIRT2-IN-20 is a SIRT2 inhibitor (human SIRT2 IC50 = 0.5 nM). SIRT2-IN-20 attenuates catalytic turnover by binding to NAD+ (HY-B0445) without forming a covalent adduct. SIRT2-IN-20 inhibits the deacetylation activity of SIRT2 and SIRT1. SIRT2-IN-20 shows cellular target engagement in live cells and induces α-tubulin hyperacetylation in cancer cells, and can be used for research on prostate cancer.
For research use only. We do not sell to patients.
- Formula: C30H57N5O4S
- Molecular Weight:583.87
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
hSIRT2 0.5 nM (IC50) |
SIRT2 40 nM (EC50) |
SIRT1 < 0.1 μM (IC50) |
SIRT3 2.3 μM (IC50) |
α-Tubulin |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | EC50 |
40 nM
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Target engagement in HEK293T cells stably expressing NanoLuc-tagged SIRT2 assessed by NanoBRET assay incubated 2 hrs.
Target engagement in HEK293T cells stably expressing NanoLuc-tagged SIRT2 assessed by NanoBRET assay incubated 2 hrs.
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acs.jmedchem.6c01275 |
In Vitro
SIRT2-IN-20 (10 μM; 5 min before thermal gradient) stabilizes SIRT2, with a thermal shift of 7.9°C when used alone and a thermal shift of 11.1°C in the presence of NAD+[1].
SIRT2-IN-20 (30-0.014 μM; 4 h) inhibits SIRT2 deacetylation with an IC50 ≪ 0.1 μM, while inhibiting SIRT1 with an IC50 < 0.1 μM and inhibiting SIRT3 with an IC50 of 2.3 μM[1].
SIRT2-IN-20 (0.1-1000 nM; 2 h) binds to SIRT2 in HEK293T cells with an EC50 of 40 nM[1].
SIRT2-IN-20 (0.1-1000 nM) inhibits SIRT2 in a concentration-dependent manner in cell-free inhibition assays.
SIRT2-IN-20 (10-30 µM; without NAD+ and with 2.5 mM NAD+) stabilizes SIRT2 at 10 and 30 µM in thermal shift assays, both without NAD+ and with 2.5 mM NAD+.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3M-Luc cells
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Concentration:0.5 μM
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Incubation Time:16 h
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Result:Induced pronounced α-tubulin hyperacetylation of the microtubule network at 0.5 μM, comparable to SH10, TSA, and SAHA.
Chemical Information
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Molecular Weight 583.87
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Formula C30H57N5O4S
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SMILES
O=C(N)[C@@H](NN[C@@H](CCCCN)C(C(C)=O)=O)CCCCNC(CC1(CC1)CSCCCCCCCCCC)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SIRT2-IN-20 Related Classifications
HY-191439 Related Classifications
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