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Tocris Bioscience™ AS 99
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Catalog No. 76485
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76-485 5 mg
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Catalog No. 76-485 Supplier Tocris Bioscience™ Supplier No. 7648/5
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Description

Selective ASH1L histone methyltransferase inhibitor

AS 99 is a selective ASH1L histone methyltransferase inhibitor (IC50 = 0.79 μM); it binds to the autoinhibitory loop region in the SET domain (Kd = 0.89 μM). AS 99 exhibits >100-fold selectivity for ASH1L over a range of lysine methyltransferases; no significant inhibition is observed at 50 μM against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. In leukemia cells, AS 99 blocks H3K36 methylation, and causes a dose-dependent downregulation of MLL fusion target genes; it also induces apoptosis and differentiation and inhibits cell proliferation. AS 99 reduces leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood count in normal mice.

Specifications

Chemical Name or Material N-[[3-[3-(Aminothioxomethyl)phenyl]-1-[1-[(trifluoromethyl)sulfonyl]-4-piperidinyl]-1 H-indol-6-yl]methyl]-1-methyl-3-azetidinecarboxamide
CAS 2323623-93-2
Quantity 5 mg
Target Lysine Methyltransferase Inhibitors
Molecular Formula C27H30F3N5O3S2
Purity 0.98
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