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Description: Selective ASH1L histone methyltransferase inhibitor
Chemical Name: N-[[3-[3-(Aminothioxomethyl)phenyl]-1-[1-[(trifluoromethyl)sulfonyl]-4-piperidinyl]-1H-indol-6-yl]methyl]-1-methyl-3-azetidinecarboxamide
Purity: ≥98% (HPLC)
Biological Activity for AS 99
AS 99 is a selective ASH1L histone methyltransferase inhibitor (IC50 = 0.79 μM); it binds to the autoinhibitory loop region in the SET domain (Kd = 0.89 μM). AS 99 exhibits >100-fold selectivity for ASH1L over a range of lysine methyltransferases; no significant inhibition is observed at 50 μM against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. In leukemia cells, AS 99 blocks H3K36 methylation, and causes a dose-dependent downregulation of MLL fusion target genes; it also induces apoptosis and differentiation and inhibits cell proliferation. AS 99 reduces leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood count in normal mice.
Licensing Information
Sold under license from the University of Michigan
Technical Data for AS 99
| M. Wt | 593.68 |
| Formula | C27H30F3N5O3S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2323623-93-2 |
| PubChem ID | 138630366 |
| InChI Key | VPQCHIWQHIOPQS-UHFFFAOYSA-N |
| Smiles | CN1CC(C(NCC2=CC=C3C(N(C4CCN(S(=O)(C(F)(F)F)=O)CC4)C=C3C5=CC(C(N)=S)=CC=C5)=C2)=O)C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AS 99
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 59.37 | 100 |
Preparing Stock Solutions for AS 99
The following data is based on the product molecular weight 593.68. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.68 mL | 8.42 mL | 16.84 mL |
| 5 mM | 0.34 mL | 1.68 mL | 3.37 mL |
| 10 mM | 0.17 mL | 0.84 mL | 1.68 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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Product Datasheets for AS 99
References for AS 99
References are publications that support the biological activity of the product.
Rogawski et al (2021) Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity. Nat.Commun 12 2792 PMID: 33990599
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Keywords: AS 99, AS 99 supplier, AS99, selective, inhibitor, inhibits, inhibitors, ASH1L, histone, methyltransferase, anti-leukemic, leukemia, MLL, H3K36, apoptosis, cell, proliferation, Other, Lysine, Methyltransferases, 7648, Tocris Bioscience
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