CC-401 HCl

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Chemical Structure| 1438391-30-0 同义名 : CC-401 Hydrochloride
CAS号 : 1438391-30-0
货号 : A101734
分子式 : C22H25ClN6O
纯度 : 99%+
分子量 : 424.926
MDL号 : MFCD21364765
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(247.1 mM)，配合低频超声助溶，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

H2O: 12 mg/mL(28.24 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 The c-Jun N-terminal kinase (JNK) signaling plays an important role in tubular cell apoptosis. CC-401 is a potent, small-molecule JNK inhibitor with Ki values of 25-50nM for three forms of JNK. It inhibits JNK in cell-based assays at a concentration of 1-5μM. CC-401 dose-dependently inhibited sorbitol-induced phosphorylation of c-Jun in HK-2 human tubular epithelial cell line at doses of 0.25-4μM. The oral administration of rats underwent unilateral ureteral obstruction with CC-401 (100mg/kg, twice daily) for 7 days reduced interstitial volume, the accumulation of α-SMA+ myofibroblasts, and collagen IV deposition as compared to the vehicle-treated group. Rats treated with CC-401 also showed reduced mRNA expressions of TGF-β1, connective tissue growth factor, and collagen IV in the kidney compared with vehicle-treated animals[3].
作用机制 CC-401 is a JNK inhibitor that competitively binds to the ATP binding site of JNK, inhibiting the phosphorylation of the N-terminal activation domain of c-Jun[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.24mL

11.77mL

2.35mL

1.18mL

23.53mL

4.71mL

2.35mL
参考文献

[1]Vasilevskaya IA, Selvakumaran M, et al. Inhibition of JNK Sensitizes Hypoxic Colon Cancer Cells to DNA-Damaging Agents. Clin Cancer Res. 2015 Sep 15;21(18):4143-52.

[2]Uehara T, Bennett B, et al. JNK mediates hepatic ischemia reperfusion injury.J Hepatol. 2005 Jun;42(6):850-9.

[3]Ma FY, Flanc RS, Tesch GH, et al. A pathogenic role for c-Jun amino-terminal kinase signaling in renal fibrosis and tubular cell apoptosis. J Am Soc Nephrol. 2007;18(2):472-484. doi:10.1681/ASN.2006060604