Tocris Bioscience™ AS 99

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