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AS-99 (free base)

AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo[1].

Product Specifications

CAS Number

2323623-93-2

UNSPSC

12352005

Target

Apoptosis; Histone Methyltransferase

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/as-99.html

Solubility

10 mM in DMSO

Smiles

O=C(C1CN(C)C1)NCC2=CC3=C(C=C2)C(C4=CC=CC(C(N)=S)=C4)=CN3C5CCN(S(=O)(C(F)(F)F)=O)CC5

Molecular Formula

C27H30F3N5O3S2

Molecular Weight

593.68

References & Citations

[1]David S. Rogawski, Jing Deng, Hao Li, Tomasz Cierpicki, Jolanta Grembecka, et al. Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity. Nat Commun. 2021 May 14;12 (1) :2792.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

ASH1L/KMT2H

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