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ML390 {[allProObj[0].p_purity_real_show]}

货号:A589360

ML390 is a human DHODH inhibitor that induces differentiation in acute myeloid leukemia.

ML390 化学结构 CAS号:2029049-79-2
ML390 化学结构
CAS号:2029049-79-2
ML390 3D分子结构
CAS号:2029049-79-2
ML390 化学结构 CAS号:2029049-79-2
ML390 3D分子结构 CAS号:2029049-79-2
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ML390 纯度/质量文件 产品仅供科研

货号:A589360 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Dehydrogenase 其他靶点 纯度
Trilostane 99+%
AGI-6780 +++

IDH2 R140Q mutant, IC50: 23 nM

99%+
Gimeracil 98%
AGI-5198 ++

R132H-IDH1, IC50: 70 nM

R132C-IDH1, IC50: 0.16 μM

99%+
SW033291 ++++

15-PGDH, IC50: 1.5 nM

15-PGDH, Ki: 0.1 nM

99%+
Mycophenolic acid 99+%
Fomepizole 98%
Leflunomide 98%
3-Nitropropanoic acid 99%+
Isovaleramide 98%
Mycophenolate Mofetil +++

Inosine monophosphate dehydrogenase I, IC50: 39 nM

Inosine monophosphate dehydrogenase II, IC50: 27 nM

98%
MK-8245 ++++

SCD1 (rat), IC50: 3 nM

SCD1 (mouse), IC50: 1 nM

99%+
Vidofludimus ++

Human DHODH, IC50: 134 nM

99%+
Emodin 98%
Ivosidenib 98%
NCT-501 ++

ALDH1A1, IC50: 40 nM

98%
Gossypol 99%+
Devimistat 98%
Disulfiram 98%+
Enasidenib ++++

IDH2, IC50: 12 nM

98%
PluriSIn 1 99%+
ML390 +

DHODH, IC50: 0.56 μM

99%+
Teriflunomide 99%+
Daidzin +++

ALDH-Ⅰ, Ki: 20 nM

98+%
18β-Glycyrrhetinic acid 99%
RRx-001 95%
NCT-503 +

PHGDH, IC50: 2.5 μM

99%+
Vorasidenib 99%+
Ammonium Glycyrrhizinate(x:1) 98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

ML390 生物活性

靶点
  • Dehydrogenase

    DHODH, IC50:0.56 μM

描述 Dihydroorotate dehydrogenase (DHODH) catalyzes the oxidation of dihydroorotate to orotate in de novo pyrimidine synthesis, e.g., uridine 5′-monophosphate. ML390 is a small-molecule probe active in overcoming differentiation arrest in a model of AML (acute myeloid leukemia). Its effect is due to inhibition of DHODH-catalyzed pyrimidine synthesis[3]. ML390 is very well-tolerated with limited cytotoxicity at high concentration when assayed against cultures of normal human primary bone marrow cells. ML390 triggers myeloid differentiation in murine and human cell line models of acute myeloid leukemia. The stability of probe ML390 in PBS (0.1% DMSO) was measured and the probe is stable as approximately 100% was present after 24 hours of incubation[4].
作用机制 The (R)-amino tetralin group of ML390 is located within the innermost part of the cavity and makes the closest contact[3].

ML390 参考文献

[1]Lewis TA, Sykes DB, et al. Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia. ACS Med Chem Lett. 2016 Sep 28;7(12):1112-1117.

[2]Sykes DB, Haynes MK, et al. Discovering Small Molecules that Overcome Differentiation Arrest in Acute Myeloid Leukemia. 2013 Dec 15 [updated 2015 Feb 11] .

[3]Lewis TA, Sykes DB, Law JM, et al. Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia. ACS Med Chem Lett. 2016;7(12):1112‐1117

[4]Sykes DB, Haynes MK, Waller A, et al. Discovering Small Molecules that Overcome Differentiation Arrest in Acute Myeloid Leukemia. In: Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD): National Center for Biotechnology Information (US); 2010

ML390 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.61mL

4.92mL

2.46mL

ML390 技术信息

CAS号2029049-79-2
分子式C21H21F3N2O3
分子量 406.398
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 25 mg/mL(61.52 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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