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关于此项目
经验公式(希尔记法):
C28H26N4O3
化学文摘社编号:
分子量:
466.53
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥97% (HPLC)
Form:
liquid
Quality level:
Storage condition:
OK to freeze, protect from light
产品名称
星形孢菌素链霉菌sp., InSolution, ≥97%, 1 mM solution, protein kinase inhibitor
Quality Level
assay
≥97% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
shipped in
wet ice
storage temp.
−70°C
SMILES string
[n]21c3c4[n](c6c(c4c7c(c3c8c2cccc8)CNC7=O)cccc6)[C@@H]5O[C@]1([C@@H]([C@@H](C5)NC)OC)C
InChI
1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
InChI key
HKSZLNNOFSGOKW-FYTWVXJKSA-N
General description
一种有效的、细胞可渗透的广谱蛋白激酶抑制剂。可抑制CaM激酶(IC50 = 20 nM)、肌球蛋白轻链激酶(IC50 = 1.3 nM)、蛋白激酶A(IC50 = 7 nM)、蛋白激酶C(IC50 = 0.7 nM)和蛋白激酶G(IC50 = 8.5 nM)。还可抑制胶原蛋白或ADP诱导的血小板凝集,但对凝血酶诱导的血小板凝集没有影响。诱导人恶性神经胶质瘤细胞系凋亡。在G1检查点对正常细胞进行阻滞。
Biochem/physiol Actions
产物与ATP竞争。
可逆性:是
细胞可渗透性:是
靶标IC50:针对蛋白激酶A、CaM激酶、肌球蛋白轻链激酶、蛋白激酶C和蛋白激酶G分别为7 nM、20 nM、1.3 nM、700 pM和8.5 nM。
首要靶标
PKA
PKA
Packaging
用惰性气体包装
Physical form
1 mM (100 µg/214 µl)星形孢菌素(目录号569397)的DMSO溶液。
Preparation Note
初始解冻后,分装,用惰性气体吹扫,然后冻存(-70°C)。
Other Notes
Couldwell, W.T., et al. 1994.FEBS Lett.345, 43.
Nishimura, H. and Simpson, I.A.1994.Biochem.J.302, 271.
Bruno, S., et al. 1992.Cancer Res.52, 470.
Kiss, Z. and Deli, E. 1992.Biochem.J.288, 853.
Vitale, M.L., et al. 1992.Neuroscience51, 463.
Hoffman, R. and Newland, E.S.1991.Cancer Chemotherap.Pharmacol.28, 102.
Oka, S., et al. 1986.Agric. Biol. Chem.50, 2723.
Nishimura, H. and Simpson, I.A.1994.Biochem.J.302, 271.
Bruno, S., et al. 1992.Cancer Res.52, 470.
Kiss, Z. and Deli, E. 1992.Biochem.J.288, 853.
Vitale, M.L., et al. 1992.Neuroscience51, 463.
Hoffman, R. and Newland, E.S.1991.Cancer Chemotherap.Pharmacol.28, 102.
Oka, S., et al. 1986.Agric. Biol. Chem.50, 2723.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性:刺激性(B)
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存储类别
10 - Combustible liquids
wgk
WGK 1
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
Erin R Spiller et al.
Frontiers in oncology, 11, 771173-771173 (2022-01-08)
Three-quarters of compounds that enter clinical trials fail to make it to market due to safety or efficacy concerns. This statistic strongly suggests a need for better screening methods that result in improved translatability of compounds during the preclinical testing
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| 569396-100UG | 07790788051693 |