货号:A199871 同义名: Gö 6983;Goe 6983
Go 6983是一种全能 PKC 抑制剂,针对 PKCα、PKCβ、PKCγ 和 PKCδ,IC50 分别为 7 nM、7 nM、6 nM 和 10 nM,对 PKCζ 的活性较低且对 PKCμ 不活跃。
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产品名称 | ALK1 ↓ ↑ | ALK2 ↓ ↑ | ALK3 ↓ ↑ | ALK4 ↓ ↑ | ALK6 ↓ ↑ | Smad3 ↓ ↑ | TGF-β ↓ ↑ | TGFβRI/ALK5 ↓ ↑ | TGFβRII ↓ ↑ | 其他靶点 | 纯度 | ||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
LDN193189 |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99%+ | ||||||||||||||
LDN-212854 |
++++
ALK1, IC50: 2.4 nM |
++++
ALK2, IC50: 1.3 nM |
+
ALK3, IC50: 85.8 nM |
+
ALK4, IC50: 2133 nM |
+
ALK5, IC50: 9276 nM |
99%+ | |||||||||||||
ML347 |
++
ALK1, IC50: 46 nM |
++
ALK2, IC50: 32 nM |
98% | ||||||||||||||||
K02288 |
++++
ALK1, IC50: 1.8 nM |
++++
ALK2, IC50: 1.1 nM |
++
ALK3, IC50: 34.4 nM |
+++
ALK6, IC50: 6.4 nM |
99%+ | ||||||||||||||
LDN-193189 dihydrochloride |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99% | ||||||||||||||
LDN-214117 |
++
ALK2, IC50: 24 nM |
98% | |||||||||||||||||
DMH-1 |
+
ALK2, IC50: 107.9 nM |
99%+ | |||||||||||||||||
SB-505124 |
+
ALK4, IC50: 129 nM |
++
ALK5, IC50: 47 nM |
99%+ | ||||||||||||||||
Vactosertib |
+++
ALK4, IC50: 13 nM |
+++
ALK5, IC50: 11 nM |
99%+ | ||||||||||||||||
Alantolactone | ✔ | 98% | |||||||||||||||||
SIS3 | ✔ | 97% | |||||||||||||||||
Pirfenidone | ✔ | 98% | |||||||||||||||||
Hesperetin | ✔ | 97% | |||||||||||||||||
RepSox |
++++
TGFβR1(ALK5), IC50: 4 nM |
98% | |||||||||||||||||
GW788388 |
+++
ALK5, IC50: 18 nM |
98% | |||||||||||||||||
LY364947 |
++
TGFβRI, IC50: 59 nM |
+
TGFβRII, IC50: 0.4 μM |
98% | ||||||||||||||||
SD-208 |
++
TGF-βRI (ALK5), IC50: 48 nM |
99% | |||||||||||||||||
SB-525334 |
+++
TGFβR1(ALK5), IC50: 14.3 nM |
99%+ | |||||||||||||||||
LY2109761 |
++
TβRI, Ki: 38 nM |
+
TβRII, Ki: 300 nM |
99%+ | ||||||||||||||||
Galunisertib |
++
TβRI, IC50: 56 nM |
98% | |||||||||||||||||
SB 431542 |
+
ALK5, IC50: 94 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | PKC ↓ ↑ | PKCα ↓ ↑ | PKCβ ↓ ↑ | PKCγ ↓ ↑ | PKCδ ↓ ↑ | PKCε ↓ ↑ | PKCζ ↓ ↑ | PKCη ↓ ↑ | PKCθ ↓ ↑ | 其他靶点 | 纯度 | ||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Daphnetin |
+
PKC, IC50: 25.01 μM |
EGFR,PKA | 95% | ||||||||||||||||
Dequalinium Chloride | 99%+ | ||||||||||||||||||
Quercetin | ✔ | Sirtuin,Src | 97% | ||||||||||||||||
Myricetrin | ✔ | 96% | |||||||||||||||||
Go 6983 |
+++
PKCα, IC50: 7 nM |
+++
PKCβ, IC50: 7 nM |
+++
PKCγ, IC50: 6 nM |
+++
PKCδ, IC50: 10 nM |
++
PKCζ, IC50: 60 nM |
99%+ | |||||||||||||
Go6976 |
+++
PKC, IC50: 7.9 nM |
++++
PKCα, IC50: 2.3 nM |
+++
PKCβ1, IC50: 6.2 nM |
FLT3 | 99%+ | ||||||||||||||
Bisindolylmaleimide I |
+++
PKCα, IC50: 20 nM |
+++
PKCβ1, IC50: 17 nM PKCβ2, IC50: 16 nM |
+++
PKCγ, IC50: 20 nM |
99%+ | |||||||||||||||
Lawsone methyl ether | ✔ | 99% | |||||||||||||||||
Sotrastaurin |
++++
PKCα, Ki: 0.95 nM |
++++
PKCβ1, Ki: 0.64 nM |
++++
PKCδ, Ki: 2.1 nM |
++++
PKCε, Ki: 3.2 nM |
++++
PKCη, Ki: 1.8 nM |
++++
PKCθ, Ki: 0.22 nM |
99%+ | ||||||||||||
Enzastaurin |
++
PKCα, IC50: 39 nM |
+++
PKCβ, IC50: 6 nM |
+
PKCγ, IC50: 83 nM |
+
PKCε, IC50: 110 nM |
98% | ||||||||||||||
Midostaurin |
++
PKCα, IC50: 22 nM |
++
PKCβ1, IC50: 30 nM PKCβ2, IC50: 31 nM |
++
PKCγ, IC50: 24 nM |
+
PKCδ, IC50: 330 nM |
+
PKCε, IC50: 1.25 μM |
+
PKCη, IC50: 160 nM |
99% | ||||||||||||
Ro 31-8220 mesylate |
++++
PKCα, IC50: 5 nM |
+++
PKCβ1, IC50: 24 nM PKCβ2, IC50: 14 nM |
++
PKCγ, IC50: 27 nM |
++
PKCε, IC50: 24 nM |
99%+ | ||||||||||||||
Staurosporine |
++++
PKCα, IC50: 2 nM |
++++
PKCγ, IC50: 5 nM |
+++
PKCδ, IC50: 20 nM |
++
PKCε, IC50: 73 nM |
++++
PKCη, IC50: 4 nM |
99%+ | |||||||||||||
Ruboxistaurin HCl |
+
PKCα, IC50: 0.36 μM |
++++
PKCβ1, IC50: 4.7 nM PKCβ2, IC50: 5.9 nM |
+
PKCγ, IC50: 0.3 μM |
+
PKCδ, IC50: 0.25 μM |
++
PKCη, IC50: 0.052 μM |
99%+ | |||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Protein kinase C (PKC) is a serine/threonine protein kinase, which plays a crucial role in signaling transduction mechanisms in many cell types and tissues. Gö 6983 is a pan-PKC inhibitor with IC50 values of 7nM, 7nM, 6nM, 10nM and 60nM (measure by protein kinase assay) for PKCα, PKCβ, PKCγ, PKCδ and PKCζ, whereas no activity against PKCμ with IC50 value of 20000nM. Gö 6983 is different with the normal pan-PKC inhibitor, such as staurosporine (IC50=40nM), for it has no effect on PKCμ, facilitating its ability to selective determination of PKCμ kinase activity in the presence of other PKC isoenzymes[1]. Treatment with Gö6983 induced the surface expression of NCRs, including NCR1, NCR2 and NCR3 (measured by relative MFI ratio) in a time- and dose-dependent manner, in primary NK cells. Pre-treatment with Gö6983 for 4h enhanced NK cell-mediated tumor cell killing at an E:T ratio of 3:1, performing as increased apoptosis and cytotoxicity on HepG2, Hep3B and HeLa cells, but has no cytotoxicity itself. Injection with 22.0ug of Gö6983 once daily on days-2, 0, 2, and 4 strongly inhibited tumor metastasis in pulmonary tumor metastasis models[2]. Inhibition of PKC through Gö 6983 could maintain ESC-specific epigenetic modifications at the chromatin domains of pluripotency genes and, thus maintain the expression of these genes in rat embryonic stem cells[3]. It was found that Gö6983 could also inhibit the activity of PfPKB, a protein kinase B homologue in Plasmodium falciparum[4]. |
作用机制 | Gö 6983 acts at the ATP binding site which is highly conserved across PKC isoforms. [5] |
Dose | Mice[6] (i.p.): 2.5 mg/kg |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.26mL 0.45mL 0.23mL |
11.30mL 2.26mL 1.13mL |
22.60mL 4.52mL 2.26mL |
CAS号 | 133053-19-7 |
分子式 | C26H26N4O3 |
分子量 | 442.51 |
别名 | Gö 6983;Goe 6983;Go6983 Go-6983 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 35 mg/mL(79.09 mM),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 |
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear PO 0.5% CMC-Na 30 mg/mL suspension |