AS-99 (TFA)

• UNSPSC 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].

• Target Antigen:

  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

• 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 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

• Clinical Information:

  No Development Reported