ASH1L inhibitor AS-99 (AS99)

Chemical Structure : ASH1L inhibitor AS-99

CAS No.: 2323623-93-2

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货号: 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.

规格	价格	库存
2 mg	￥2480	In stock
5 mg	￥3980	In stock
10 mg	￥5980	In stock
25 mg		Get quote
100 mg		Get quote

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生物&药学活性

ASH1L inhibitor AS-99 (AS99) 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.

物理化学性质&存储条件

分子量	593.684
分子式	C27H30F3N5O3S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
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-

参考文献

1. David S Rogawski, et al. Nat Commun. 2021 May 14;12(1):2792.