Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : ASH1L inhibitor AS-99
CAS No.: 2323623-93-2
Catalog No.: PC-72494Not For Human Use, Lab Use Only.
ASH1L inhibitor AS-99 (AS-99) is a first-in-class, potent, selective inhibitor of ASH1L histone methyltransferase with IC50 of 0.79 uM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $298 | In stock | |
| 5 mg | $498 | In stock | |
| 10 mg | $758 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
ASH1L inhibitor AS-99 (AS-99) is a first-in-class, potent, selective inhibitor of ASH1L histone methyltransferase with IC50 of 0.79 uM.
AS-99 strongly bind to the ASH1L SET domain with Kd values of 0.89 uM.
AS-99 displayed no significant inhibition (>100-fold selectivity) at 50 uM against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2.
AS-99 inhibits the growth of leukemia cells (MV4;11, MOLM13, and KOPN8) harboring different MLL1 translocations with the GI50 values of 1.8-3.6 uM, showed a several fold weaker effect on the proliferation of leukemia cells without MLL1 translocations, such as SET2 and K562, without toxicity in normal cells.
AS-99 impairs transcriptional program of MLL fusion proteins and reduces leukemia burden.
AS-99 reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice.
| M.Wt | 593.684 | |
| Formula | C27H30F3N5O3S2 | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
3-Azetidinecarboxamide, N-[[3-[3-(aminothioxomethyl)phenyl]-1-[1-[(trifluoromethyl)sulfonyl]-4-piperidinyl]-1H-indol-6-yl]methyl]-1-methyl- |
|
1. David S Rogawski, et al. Nat Commun. 2021 May 14;12(1):2792.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
