AS-99 (free base)

• Description :

  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].

• 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

• CAS Number :

  [2323623-93-2]