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NQDI-1 纯度: 95.93%
NQDI-1 抑制凋亡信号调节激酶 1 (ASK1),Ki 为 500 nM,IC50 为 3 μM。
![NQDI-1 Chemical Structure NQDI-1](http://www.fluoroprobe.com/wp-content/uploads/2022/05/hy-19566.gif)
NQDI-1 Chemical Structure
CAS No. : 175026-96-7
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥792 | In-stock | |
5 mg | ¥720 | In-stock | |
10 mg | ¥1200 | In-stock | |
50 mg | ¥4000 | In-stock | |
100 mg | ¥7500 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
NQDI-1 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Apoptosis Compound Library
- Immunology/Inflammation Compound Library
- Kinase Inhibitor Library
- MAPK Compound Library
- Anti-Cancer Compound Library
- Oxygen Sensing Compound Library
生物活性 |
NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a Ki of 500 nM and an IC50 of 3 μM. |
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IC50 & Target |
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体外研究 (In Vitro) |
The selectivity of NQDI-1 is evaluated in vitro on four serine/threonine protein kinases (protein kinase CK2 (CK2), c-Jun N-terminal kinase 3 (JNK3), Rho-associated protein kinase 1 (Rock1), and Aurora A) and three tyrosine protein kinases (FGFR1, hHGFR, and endothelial TEK tyrosine kinase (Tie2)). The results show that NQDI-1 is a selective inhibitor of ASK1. The activity of FGFR1 protein kinase is inhibited by NQDI-1 (residual activity of 44%). NQDI-1 inhibits ASK1 with a Ki of 500 nM. Inhibition of ASK1 by NQDI-1 is competitive with respect to the phosphodonor substrate ATP[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
250 nmol NQDI-1 in DMSO is intracerebroventricularly injected following brain insult. Western blotting is performed to determine the expression of ASK1 in the sham, Hypoxia-ischemia (HI), DMSO and NQDI-1 groups and indicate that NQDI-1 markedly inhibits the expression of ASK1 in the brain cortex, compared with the HI and DMSO group. Furthermore, immunofluorescence staining also indicates that the expression of ASK1 is inhibited by NQDI-1 in the brain cortex. The expression of downstream targets of ASK1 is also determined in the present study. The expression levels of p-JNK, p-c-Jun, p53 and caspase 3 are significantly decreased by NQDI-1, compared with the HI and DMSO groups. Low expression of p-JNK in the brain cortex is also observed by immunofluorescence in the NQDI-1-treated group[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
319.31 |
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Formula |
C19H13NO4 |
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CAS 号 |
175026-96-7 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 10 mg/mL (31.32 mM; Need ultrasonic and warming) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Kinase Assay [1] |
Enzyme activity of human protein kinases ASK1, Aurora A, ROCK1, HGFR, FGFR1, Tie2, JNK3, and CK2 is determined using in vitro kinase assay (γ-32P-ATP method). Each reaction mixture contains 6 μL of buffer solution (25 mM MOPS, pH 7.2, 2.5 mM EGTA, 2.5 mM EDTA, 0.5 mM DTT, 0.25 mg/mL BSA, 20 mM β-glycerophosphate), 3 μL of substrate solution (MBP, Long S6 kinase substrate peptide, KKKSPGEYVNIEFG, IGF-IRtide (12-527), TK substrate 2, JNK3tide, or RRRDDDSDDD for each kinase, respectively) (5.0 μg/μL), 0.3 μL of enzyme (protein kinase catalytic subunit, 0.1 μg/μL≈32 mU/μL), and 10.25 μL of H2O. The reaction mixture (total volume of 19 μL) is quickly added to 1.5 mL tubes at room temperature. The stock solutions of inhibitors (e.g., NQDI-1) are prepared in DMSO, and the concentration of inhibitor is 1 mM. The concentration of DMSO in the reaction does not exceed 3%. Then 1 μL of inhibitor solution in DMSO is added to each tube and mixed by pipetting. ATP solution is prepared separately. For each sample 0.05 mCi γ-[P32]ATP is taken (specific activity of 100 μCi/μM). The total concentration of labeled and unlabeled ATP is 100 μM. The reaction is started with addition of ATP solution (150 μM ATP, 30 mM MgCl2, 15 mM MOPS, pH 7.2). The time of reaction is 20 min at 30°C. The reaction is stopped by adding 20 μL of 0.5 M orthophosphoric acid. Then the reaction mixture is loaded on the 20 mm filter disks of the cellulose phosphate paper. Filters are washed three times with 0.075 M orthophosphoric acid at room temperature and dried. For detection of products, dried filters are counted by Tri-Carb 2800-TR liquid scintillation analyzer. Then 1 μL of DMSO is added to the reaction volume instead of the inhibitor stock solution for a positive control[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [2] |
Rats[2] 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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