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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。 |
靶点 |
|
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]. |
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 |
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 |