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经验公式(希尔记法):
C25H24N4O2 · HCl
化学文摘社编号:
分子量:
448.94
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
GF 109203X 盐酸盐, ≥95%
InChI
1S/C25H24N4O2.ClH/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20;/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31);1H
SMILES string
Cl.CN(C)CCCn1cc(C2=C(C(=O)NC2=O)c3c[nH]c4ccccc34)c5ccccc15
InChI key
XRAMWNCMYJHGGH-UHFFFAOYSA-N
biological source
synthetic (organic)
assay
≥95%
form
solid
solubility
methanol: 10 mg/mL, clear, orange to red
storage temp.
2-8°C
Quality Level
相关类别
Application
GF 109203X盐酸盐已被用于在人神经母细胞瘤衍生的kelly细胞中抑制蛋白激酶C。
Biochem/physiol Actions
蛋白激酶C的抑制剂;GSK-3的有效抑制剂。
General description
GF 109203X可防止胶原蛋白触发的腺苷和三磷酸(ATP)分泌。它还可抑制胶原蛋白和α-凝血酶诱导的血小板聚集。它可作为糖原合成酶激酶-3(GSK-3)的抑制剂。GF 109203X也可作为一种抗炎剂。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C
Toullec D1, et al.
The Journal of Biological Chemistry, 266(24), 15771-15781 (1991)
Phorbol-ester mediated suppression of hASH1 synthesis: multiple ways to keep the level down
Benko E, et al.
Frontiers in Molecular Neuroscience, 4(1), 1-1 (2011)
Anti-inflammatory properties of the protein kinase C inhibitor, 3-[1-[3-(dimethylamino) propyl]-1H-indol-3-yl]-4 (1H-indol-3-yl)-1H-pyrrole-2, 5-dione monohydrochloride (GF109203X) in the PMA-mouse ear edema model
Kuchera S, et al.
Agents and Actions, 39(1), C169-C173 (1993)
The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity
Hers I, et al.
Febs Letters, 460(3), 433-436 (1999)
D Toullec et al.
The Journal of biological chemistry, 266(24), 15771-15781 (1991-08-25)
Staurosporine is the most potent inhibitor of protein kinase C (PKC) described in the literature with a half-maximal inhibitory concentration (IC50) of 10 nM. Nevertheless, this natural product is poorly selective when assayed against other protein kinases. In order to
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