Sotrastaurin (AEB071) 是一种高效且口服活性的泛 PKC 抑制剂,对 PKCθ、PKCβ、PKCα、PKCη、PKCδ 和 PKCε 的 Ki 值分别为 0.22 nM、0.64 nM、0.95 nM、1.8 nM、2.1 nM 和 3.2 nM。
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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 |
99%+ | ||||||||||||||||
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 | ✔ | 99%+ | |||||||||||||||||
Hesperetin | ✔ | 98%+ | |||||||||||||||||
RepSox |
++++
TGFβR1(ALK5), IC50: 4 nM |
99%+ | |||||||||||||||||
GW788388 |
+++
ALK5, IC50: 18 nM |
99%+ | |||||||||||||||||
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 | 99%+ | ||||||||||||||||
Dequalinium Chloride | 99%+ | ||||||||||||||||||
Quercetin | ✔ | Src,Sirtuin | 97% | ||||||||||||||||
Myricetrin | ✔ | 97%+ | |||||||||||||||||
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 |
99%+ | ||||||||||||||
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. Sotrastaurin (AEB071), as an immuno- suppressor, is a pan selective PKC inhibitor with Ki value of 0.95 nM, 0.64 nM, 2.1 nM, 3.2 nM, 1.8 nM and 0.22 nM for PKCα, PKCβ1, PKCδ, PKCε, PKCη and PKCθ (measured by scintillation proximity assay technology). Sotrastaurin suppresses T-cell activation, in a complementary and different manner to calcineurin inhibitor such as cyclosporine A. Sotrastaurin can effectively abrogate CD3/CD28 antibody and alloantigen-driven T-cell responses. Treatment with sotrastaurin at a concentration of 250 nM can markedly decrease proliferation responses induced by antibody- or phorbol ester treatment in mouse CD3 T cells. Both IL-2 and IFNγ levels were strongly inhibited by sotrastaurin (<1000 nM) in the transgenic TCR DO11.10 mouse CD4+ T cells after physiological stimulation with the antigenic OVA peptide. This inhibition on T cells may due to the suppression on the canonical NF-κB and NFAT transactivation pathway. Sotrastaurin strongly inhibited phorbol ester-induced adhesion responses of Jurkat cells with an IC50 value of 300 nM, in stark contrast with CsA treatment inactive up to 1 μM in this assay[1]. The almost completed inhibition of Sotrastaurin on CD25 expression was achieved at 2h, with >60% inhibition remaining 6h after administration in the T lymphocytes activated by anti-CD28 antibody in combination with PMA, from Lewis rats treated with a single oral dose of sotrastaurin on 30 mg/kg[2]. Oral administration of sotrastaurin on 30 mg/kg, b.i.d, showed immunosuppressive effect and led to pronounced prolongation survival in rats with heart allograft[2]. Sotrastaurin is being developed as an immunosuppressive for organ transplantation. Up to now, several phase 2 studies on efficacy, safety and tolerability of sotrastaurin on transplantation have been completed (see https://clinicaltrials.gov/). |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
92.1 | 0.5 μM | Growth Inhibition Assay | 3 h | enhances IR-induced reduction in cell viability | 24595385 |
92.1 | 0.5 μM | Growth Inhibition Assay | 3 h | increases IR-induced cell cycle arrest | 24595385 |
92.1 | 0-5 μM | Growth Inhibition Assay | 72 h | inhibits cell growth dose dependently | 22653968 |
92.1 | 5 μM | Growth Inhibition Assay | 24 h | induces G1 arrest | 22653968 |
Dose | Mice[3] (p.o.): 80 mg/kg; rat[2] (p.o.): 3 mg/kg - 10 mg/kg | ||||||||||||||||||
Administration | p.o. | ||||||||||||||||||
Pharmacokinetics |
|
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.28mL 0.46mL 0.23mL |
11.40mL 2.28mL 1.14mL |
22.81mL 4.56mL 2.28mL |
CAS号 | 425637-18-9 |
分子式 | C25H22N6O2 |
分子量 | 438.481 |
别名 | AEB071 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 50 mg/mL(114.03 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 |
2% DMSO+30% PEG 300+water 10 mg/mL |