AS-99 (TFA)
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].
Product Specifications
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
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.
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