AS 99

Product Description

AS 99 is a selective ASH1L histone methyltransferase inhibitor (IC₅₀ = 0.79 μM); it binds to the autoinhibitory loop region in the SET domain (K_d = 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.

Licensing Information

Sold under license from the University of Michigan

Solubility

Preparing Stock Solutions for AS 99

The following data is based on the product molecular weight 593.68

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.68 mL	8.42 mL	16.84 mL
5 mM	0.34 mL	1.68 mL	3.37 mL
10 mM	0.17 mL	0.84 mL	1.68 mL
50 mM	0.03 mL	0.17 mL	0.34 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Rogawski Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity. Nat.Commun 2021 PMID: 33990599