Maleic acid is used in the synthesis of pyridoindolones as potent inhibitors of Aurora kinases. It is a reagent in the preparation of TiO2/carbon nanotube composites.
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产品名称 | Aurora A ↓ ↑ | Aurora B ↓ ↑ | Aurora C ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BI-847325 |
++
Aurora A (Human), IC50: 25 nM |
++++
Aurora B (Xenopus laevis), IC50: 3 nM |
++
Aurora C (Human), IC50: 15 nM |
99%+ | |||||||||||||||
CCT 137690 |
++
Aurora A, IC50: 15 nM |
++
Aurora B, IC50: 25 nM |
++
Aurora C, IC50: 19 nM |
99%+ | |||||||||||||||
MK-5108 |
++++
Aurora A, IC50: 0.064 nM |
99%+ | |||||||||||||||||
KW-2449 |
+
Aurora A, IC50: 48 nM |
FLT3 | 99%+ | ||||||||||||||||
Tozasertib |
++++
Aurora A, Ki app: 0.6 nM |
++
Aurora B, Ki app: 18 nM |
+++
Aurora C, Ki app: 4.6 nM |
Bcr-Abl,FLT3 | 99%+ | ||||||||||||||
AT9283 |
++++
Aurora A, IC50: ~3.0 nM |
++++
Aurora B, IC50: ~3.0 nM |
99%+ | ||||||||||||||||
MLN8054 |
+++
Aurora A, IC50: 4 nM |
+
Aurora B, IC50: 172 nM |
99%+ | ||||||||||||||||
ZM-447439 |
+
Aurora A, IC50: 110 nM |
+
Aurora B, IC50: 130 nM |
Src | 99%+ | |||||||||||||||
TCS7010 |
++++
Aurora A, IC50: 3.4 nM |
99%+ | |||||||||||||||||
TAK-901 |
++
Aurora A-TPX2, IC50: 21 nM |
++
Aurora B-INCENP, IC50: 15 nM |
99%+ | ||||||||||||||||
Danusertib |
+++
Aurora A, IC50: 13 nM |
+
Aurora B, IC50: 79 nM |
+
Aurora C, IC50: 61 nM |
RET | 99%+ | ||||||||||||||
MK-8745 |
++++
Aurora A, IC50: 0.6 nM |
99+% | |||||||||||||||||
PHA-680632 |
++
Aurora A, IC50: 27 nM |
+
Aurora B, IC50: 135 nM |
+
Aurora C, IC50: 120 nM |
FLT3 | 99%+ | ||||||||||||||
AMG 900 |
+++
Aurora A, IC50: 5 nM |
+++
Aurora B, IC50: 4 nM |
++++
Aurora C, IC50: 1 nM |
99%+ | |||||||||||||||
Alisertib |
++++
Aurora A, IC50: 1.2 nM |
99%+ | |||||||||||||||||
ENMD-2076 |
+++
Aurora A, IC50: 14 nM |
+
Aurora B, IC50: 350 nM |
FLT3,RET | 98% | |||||||||||||||
JNJ-7706621 |
+++
Aurora A, IC50: 11 nM |
++
Aurora B, IC50: 15 nM |
99%+ | ||||||||||||||||
CYC-116 |
+++
Aurora A, Ki: 8 nM |
+++
Aurora B, Ki: 9 nM |
FLT3 | 99%+ | |||||||||||||||
Reversine |
+++
Aurora A, IC50: 12 nM |
+++
Aurora B, IC50: 13 nM |
++
Aurora C, IC50: 20 nM |
98% | |||||||||||||||
CCT129202 |
++
Aurora A, IC50: 42 nM |
+
Aurora B, IC50: 198 nM |
+
Aurora C, IC50: 227 nM |
98% | |||||||||||||||
SNS-314 mesylate |
+++
Aurora A, IC50: 9 nM |
++
Aurora B, IC50: 31 nM |
++++
Aurora C, IC50: 3 nM |
99%+ | |||||||||||||||
Barasertib-HQPA |
++++
Aurora B, IC50: 0.37 nM |
99%+ | |||||||||||||||||
Hesperadin |
+
Aurora B (human), IC50: 250 nM |
98% | |||||||||||||||||
GSK-1070916 |
++++
Aurora B-INCENP, IC50: 3.5 nM |
+++
Aurora C-INCENP, IC50: 6.5 nM |
Tie-2,SIK | 99% | |||||||||||||||
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。 |
描述 | Maleic Acid is a Glutamate Decarboxylase (GAD) inhibitor of E. coli and L. monocytogenes[3]. Maleic acid affected the extracellular GABA levels while it did not affect the intracellular ones. Maleic acid had a major impact mainly on GadD2 activity as also shown in cell lysates. Furthermore, it was demonstrated that maleic acid is able to partly remove biofilms of L. monocytogenes. Maleic acid is able to inhibit the GAD of L. monocytogenes significantly enhancing its sensitivity to acidic conditions and together with its ability to remove biofilms[4]. Maleic acid induced concentration-dependent and time-dependent cell death shown by increased lactate dehydrogenase release as well as ethidium homodimer and calcein acetoxymethyl ester staining. MA (Maleic acid) toxicity was critically dependent on calcium levels in culture medium and blocked by the extra- and intracellular calcium chelators EGTA and BAPTA-AM respectively. Moreover, MA-induced cell death was associated with activation of calcium-dependent calpain proteases[5]. MA induced proteinuria, an increase in urinary excretion of N-acetyl-β-d-glucosaminidase, and a decrease in plasma glutathione peroxidase activity, renal blood flow, and oxygenation and perfusion of renal cortex. Moreover, MA impaired mitochondrial bioenergetics associated to complex I, mitochondrial membrane potential and respiratory control index and increased the mitochondrial production of hydrogen peroxide[6]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02731287 | Hemangioma | Phase 2 | Completed | - | Spain ... 展开 >> Hospital de la Santa Creu i Sant Pau Barcelona, Spain, 08025 Hospital Virgen del Rocío Sevilla, Spain, 41013 收起 << |
NCT01873131 | Hemangioma | Not Applicable | Recruiting | December 2020 | United States, Massachusetts ... 展开 >> Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 Contact: Thanh Nga T Tran, MD PhD 617-724-4937 ttran2@partners.org Contact: Ray H Jalian, MD 617 724-4937 hjalian@partners.org Principal Investigator: R. Rox Anderson, MD Sub-Investigator: Thanh Nga T Tran, MD PhD Sub-Investigator: Kelly Stankiewicz, MD Sub-Investigator: Ray H Jalian, MD 收起 << |
NCT02207621 | Ocular Hypertension ... 展开 >> Open-angle Glaucoma 收起 << | Phase 3 | Completed | - | United States, New Jersey ... 展开 >> Aerie Pharmaceuticals Bedminster, New Jersey, United States, 07921 收起 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
8.62mL 1.72mL 0.86mL |
43.08mL 8.62mL 4.31mL |
86.15mL 17.23mL 8.62mL |
CAS号 | 110-16-7 |
分子式 | C4H4O4 |
分子量 | 116.07 |
SMILES Code | O=C(O)/C=C\C(O)=O |
MDL No. | MFCD00063177 |
别名 | 顺丁烯二酸 |
运输 | 蓝冰 |
InChI Key | VZCYOOQTPOCHFL-UPHRSURJSA-N |
Pubchem ID | 444266 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |