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AS 99

Cat. No. 7648 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Selective ASH1L histone methyltransferase inhibitor
化学名： N-[[3-[3-(Aminothioxomethyl)phenyl]-1-[1-[(trifluoromethyl)sulfonyl]-4-piperidinyl]-1H-indol-6-yl]methyl]-1-methyl-3-azetidinecarboxamide
纯度： ≥98% (HPLC)
说明书
引用文献
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生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 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.

许可信息

Sold under license from the University of Michigan

技术数据 for AS 99

分子量 593.68
公式 C27H30F3N5O3S2
储存 Store at -20°C
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for AS 99

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 59.37 100

制备储备液 for AS 99

以下数据基于产品分子量 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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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参考文献 for AS 99

参考文献是支持产品生物活性的出版物。

Rogawski et al (2021) Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity. Nat.Commun 12 2792 PMID: 33990599

If you know of a relevant reference for AS 99, please let us know.

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关键词: 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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