AS-99 (TFA)

• Description :

  AS-99 TFA 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 TFA 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-tfa.html

• Purity :

  99.15

• Solubility :

  DMSO : 100 mg/mL (ultrasonic) |H2O : 12.5 mg/mL (ultrasonic)

• 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.O=C(O)C(F)(F)F

• Molecular Formula :

  C29H31F6N5O5S2

• Molecular Weight :

  707.71

• 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 :

  Blue Ice

• Storage Conditions :

  -20°C (Powder, protect from light, stored under nitrogen)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  ASH1L/KMT2H

• Citation 01 :

  Nat Commun. 2025 May 20;16 (1) :4681.|Adv Sci (Weinh) . 2024 Dec;11 (45) :e2404756.