13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 5mg 10mg 50mg |
| CAS | 899805-25-5 |
| 別名 | Tanzisertib;CC930;CC 930 |
| 化學名 | 4-[[9-[(3S)-oxolan-3-yl]-8-(2,4,6-trifluoroanilino)purin-2-yl]amino]cyclohexan-1-ol |
| 分子式 | C21H23F3N6O2 |
| 分子量 | 448.44 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 20 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH7.2)(1:20): 0.05 mg/ml |
| 儲存條件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述：
JNKs (c-Jun N-terminal kinases) belong to kinases which were originally indentified. They bind to c-Jun then phosphorylate it on Ser-63 and Ser-73 which located in its transcriptional activation domain. JNKs belong to MAPK family. They contain ten isforms encoded by three genes: JNK1, JNK2 and JNK3. They are 46 KD or 55 KD protein. They play an important role in stress stimuli, such as heat shock, cytokines, and osmotic shock. They are also responsive to the cellular apoptosis pathway and T cell differentiation. They are activated through a dual phosphorylation of Thr and Tyr residues within a Thr-Pro-Tyr motif which located in kinase subdomain. JNKs modify the activity of many proteins that act in the nucleus reside or at the mitochondria. JNKs activate the downstream molecules which include p53, c-Jun, ELK1, SMAD4 and HSF1. JNKs regulate several important cellular functions, such as cell growth, survival, differentiation and apoptosis.[2]
CC-930 kinetically competitive with ATP in the phosphorylation of the substrate c-Jun against all isoforms of JNK with Ki values of 44 ± 3 nM (JNK1), 6.2 ± 0.6 nM and IC50 value of 5 nm for JNK3. EGFR is the only non-MAP kinase which inhibited more than 50% at 3 M. It did not inhibit greater than 50% against 22 diverse non-kinase enzymes at 10 M.[1] CC-930 reduced the phosphorylation of c-Jun the stimulated by TGF β at 1 μM which is a clinically relevant concentration in fi broblasts[3] CC-930 also was showed the potent antifibrotic founctions in the TSK1 model. CC-930 reduced hypodermal thickening with a dose-dependent manner by up to 85±4% in TSK1 mice.[3] CC-930 has no effect on kidney hypertrophy, blood pressur, podocyte loss, glomerular fibrosis in diabetic spontaneously hypertensive rats (SHR). However, CC-930 reduced the levels of ccl2 mRNA in diabetic kidneys[4].
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原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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