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Chemical Structure : A-366
CAS No.: 1527503-11-2
Catalog No.: PC-43110Not For Human Use, Lab Use Only.
A-366 is a potent, highly selective inhibitor of histone methyltransferase G9a/GLP with IC50 of 3/38 nM, >1,000-fold selectivity for G9a over 21 other methyltransferases.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $88 | In stock | |
| 25 mg | $138 | In stock | |
| 50 mg | $218 | In stock | |
| 100 mg | Get quote |
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A-366 is a potent, highly selective inhibitor of histone methyltransferase G9a/GLP with IC50 of 3/38 nM, >1,000-fold selectivity for G9a over 21 other methyltransferases.
A-366 effects a clear reduction in H3K9 methylation in cells, shows significantly less cytotoxic effects on the growth of tumor cell lines compared to other known G9a/GLP small molecule inhibitors despite equivalent cellular activity on methylation of H3K9me2 (H3K9me2 cellular EC50=0.3 uM).
A-366 induces differentiation and affects viability in MV4;11 cells, demonstrates growth inhibition in vivo consistent with the profile of H3K9me2 reduction in flank xenograft leukemia model.
| M.Wt | 329.4366 | |
| Formula | C19H27N3O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Spiro[cyclobutane-1,3'-[3H]indol]-2'-amine, 5'-methoxy-6'-[3-(1-pyrrolidinyl)propoxy]- |
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1. Sweis RF, et al. ACS Med Chem Lett. 2014 Jan 2;5(2):205-9.
2. Pappano WN, et al. PLoS One. 2015 Jul 6;10(7):e0131716.
3. Agarwal P, et al. Cancer Lett. 2016 Oct 1;380(2):467-75.
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