Inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively). Abrogates G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition. Potentiates cytotoxicity of DNA-damaging drugs, enhancing the efficacy of some chemotherapeutics.
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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 |
PKA,EGFR | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Dequalinium Chloride | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||||
Quercetin | ✔ | Src,Sirtuin | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Myricetrin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Go 6983 |
+++
PKCα, IC50: 7 nM |
+++
PKCβ, IC50: 7 nM |
+++
PKCγ, IC50: 6 nM |
+++
PKCδ, IC50: 10 nM |
++
PKCζ, IC50: 60 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||
Go6976 |
+++
PKC, IC50: 7.9 nM |
++++
PKCα, IC50: 2.3 nM |
+++
PKCβ1, IC50: 6.2 nM |
FLT3 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||
Bisindolylmaleimide I |
+++
PKCα, IC50: 20 nM |
+++
PKCβ2, IC50: 16 nM PKCβ1, IC50: 17 nM |
+++
PKCγ, IC50: 20 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
Lawsone methyl ether | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
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 |
{[allProObj[0].p_purity_real_show]} | ||||||||||||
Enzastaurin |
++
PKCα, IC50: 39 nM |
+++
PKCβ, IC50: 6 nM |
+
PKCγ, IC50: 83 nM |
+
PKCε, IC50: 110 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||
Midostaurin |
++
PKCα, IC50: 22 nM |
++
PKCβ2, IC50: 31 nM PKCβ1, IC50: 30 nM |
++
PKCγ, IC50: 24 nM |
+
PKCδ, IC50: 330 nM |
+
PKCε, IC50: 1.25 μM |
+
PKCη, IC50: 160 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||
Ro 31-8220 mesylate |
++++
PKCα, IC50: 5 nM |
+++
PKCβ2, IC50: 14 nM PKCβ1, IC50: 24 nM |
++
PKCγ, IC50: 27 nM |
++
PKCε, IC50: 24 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||
Staurosporine |
++++
PKCα, IC50: 2 nM |
++++
PKCγ, IC50: 5 nM |
+++
PKCδ, IC50: 20 nM |
++
PKCε, IC50: 73 nM |
++++
PKCη, IC50: 4 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||
Ruboxistaurin HCl |
+
PKCα, IC50: 0.36 μM |
++++
PKCβ2, IC50: 5.9 nM PKCβ1, IC50: 4.7 nM |
+
PKCγ, IC50: 0.3 μM |
+
PKCδ, IC50: 0.25 μM |
++
PKCη, IC50: 0.052 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||
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 | 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 |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||
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 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||
ML347 |
++
ALK1, IC50: 46 nM |
++
ALK2, IC50: 32 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
K02288 |
++++
ALK1, IC50: 1.8 nM |
++++
ALK2, IC50: 1.1 nM |
++
ALK3, IC50: 34.4 nM |
+++
ALK6, IC50: 6.4 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||
LDN-193189 dihydrochloride |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||
LDN-214117 |
++
ALK2, IC50: 24 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
DMH-1 |
+
ALK2, IC50: 107.9 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SB-505124 |
+
ALK4, IC50: 129 nM |
++
ALK5, IC50: 47 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Vactosertib |
+++
ALK4, IC50: 13 nM |
+++
ALK5, IC50: 11 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Alantolactone | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SIS3 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Pirfenidone | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Hesperetin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
RepSox |
++++
TGFβR1(ALK5), IC50: 4 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
GW788388 |
+++
ALK5, IC50: 18 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
LY364947 |
++
TGFβRI, IC50: 59 nM |
+
TGFβRII, IC50: 0.4 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
SD-208 |
++
TGF-βRI (ALK5), IC50: 48 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SB-525334 |
+++
TGFβR1(ALK5), IC50: 14.3 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
LY2109761 |
++
TβRI, Ki: 38 nM |
+
TβRII, Ki: 300 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Galunisertib |
++
TβRI, IC50: 56 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SB 431542 |
+
ALK5, IC50: 94 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
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 | Chk1 ↓ ↑ | Chk2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Rabusertib |
++
Chk1, IC50: 7 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
PF-477736 |
++++
Chk1, Ki: 0.49 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Prexasertib 2HCl |
++++
Chk1, Ki: 0.9 nM |
++
Chk2, IC50: 8 nM |
RSK | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
AZD-7762 |
+++
Chk1, IC50: 5 nM |
++
Chk2, IC50: <10 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
CHIR-124 |
++++
Chk1, IC50: 0.3 nM |
GSK-3,FLT3,PDGFR | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
SCH900776 |
+++
Chk1, IC50: 3 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SAR-020106 |
+
Chk1, IC50: 13.3 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
CCT245737 |
+++
Chk1, IC50: 1.4 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
BML-277 |
+
Chk2, IC50: 15 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
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 | Cdc ↓ ↑ | CDK1 ↓ ↑ | CDK19 ↓ ↑ | CDK2 ↓ ↑ | CDK3 ↓ ↑ | CDK4 ↓ ↑ | CDK5 ↓ ↑ | CDK6 ↓ ↑ | CDK7 ↓ ↑ | CDK8 ↓ ↑ | CDK9 ↓ ↑ | CLK ↓ ↑ | 其他靶点 | 纯度 | |||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
XL413 hydrochloride |
++++
Cdc7, IC50: 3.4 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SU9516 |
+++
CDK1, IC50: 40 nM |
+++
CDK2, IC50: 22 nM |
++
CDK4, IC50: 200 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
RO-3306 |
+++
CDK1, Ki: 20 nM |
ERK,SGK | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
R547 |
++++
CDK1/CyclinB, Ki: 2 nM |
++++
CDK2/CyclinE, Ki: 3 nM |
++++
CDK4/CyclinD1, Ki: 1 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
BMS-265246 |
++++
CDK1/CyclinB, IC50: 6 nM |
++++
CDK2/CyclinE, IC50: 9 nM |
+
CDK4/CyclinD, IC50: 230 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
NU6027 |
+
CDK1, Ki: 2.5 μM |
+
CDK2, Ki: 1.3 μM |
DNA-PK | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
Purvalanol A |
++++
Cdc2/CyclinB, IC50: 4 nM |
+++
CDK2/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 nM |
+
CDK4/CyclinD1, IC50: 850 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
SCH900776 |
++
CDK2, IC50: 0.16 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
AUZ 454 |
++++
CDK2(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
A-674563 HCl |
++
CDK2, Ki: 46 nM |
PKA | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
JNJ-7706621 |
++++
CDK1/CyclinB, IC50: 9 nM |
++++
CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 nM |
++
CDK3/CyclinE, IC50: 58 nM |
+
CDK4/CyclinD1, IC50: 253 nM |
++
CDK6/CyclinD1, IC50: 175 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||
AT7519 |
++
CDK1/CyclinB, IC50: 210 nM |
++
CDK2/CyclinA, IC50: 47 nM |
+
CDK3/CyclinE, IC50: 360 nM |
++
CDK4/CyclinD1, IC50: 100 nM |
+++
CDK5/p35, IC50: 13 nM |
++
CDK6/CyclinD3, IC50: 170 nM |
++++
CDK9/CyclinT, IC50: <10 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||
PHA-793887 |
++
CDK1/CyclinB, IC50: 60 nM |
++++
CDK2/CyclinE, IC50: 8 nM CDK2/CyclinA, IC50: 8 nM |
++
CDK4/CyclinD1, IC50: 62 nM |
++++
CDK5/p25, IC50: 5 nM |
++++
CDK7/CyclinH, IC50: 10 nM |
++
CDK9/CyclinT1, IC50: 138 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||
Milciclib |
+
CDK1/CyclinB, IC50: 398 nM |
++
CDK2/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM |
++
CDK4/CyclinD1, IC50: 160 nM |
+
CDK5/p35, IC50: 265 nM |
++
CDK7/CyclinH, IC50: 150 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||
Kenpaullone |
+
CDK1/CyclinB, IC50: 0.4μM |
+
CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM |
+
CDK5/p35, IC50: 0.85μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
SNS-032 |
+++
CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 nM |
+
CDK5/p35, IC50: 340 nM |
++
CDK7/CyclinH, IC50: 62 nM |
++++
CDK9/CyclinT, IC50: 4 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||
Dinaciclib |
++++
CDK1, IC50: 3 nM |
++++
CDK2, IC50: 1 nM |
++++
CDK5, IC50: 1 nM |
++++
CDK9, IC50: 4 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||
PHA-767491 hydrochloride |
++++
Cdc7, IC50: 10 nM |
+
CDK1, IC50: 250 nM |
+
CDK2, IC50: 240 nM |
+
CDK5, IC50: 460 nM |
+++
CDK9, IC50: 34 nM |
MK2 | {[allProObj[0].p_purity_real_show]} | ||||||||||||
(R)-Roscovitine |
+
Cdc2/CyclinB, IC50: 0.65 μM |
+
CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, IC50: 0.7 μM |
++
CDK5/p35, IC50: 0.16 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
Narazaciclib |
++++
CDK4/CyclinD1, IC50: 3.87 nM |
++++
CDK6/CyclinD1, IC50: 9.82 nM |
RET | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
Palbociclib |
++++
CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM |
+++
CDK6/CyclinD2, IC50: 15 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Abemaciclib |
++++
CDK4, IC50: 2 nM |
++++
CDK6, IC50: 10 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Ribociclib |
++++
CDK4, IC50: 10 nM |
+++
CDK6, IC50: 39 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Palbociclib isethionate |
++++
CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM |
+++
CDK6/CyclinD2, IC50: 15 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
BS-181 HCl |
+++
CDK7, IC50: 21 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
(E/Z)-THZ1 dihydrochloride |
++++
CDK7, IC50: 3.2 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
LDC4297 |
++++
CDK7, IC50: 0.13 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Senexin A |
+
CDK19, Kd: 0.31 μM |
+
CDK8, Kd: 0.83 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
MSC2530818 |
++++
CDK8, IC50: 2.6 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Wogonin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Riviciclib HCl |
++
CDK1/CyclinB, IC50: 79 nM |
+
CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM |
++
CDK4/CyclinD1, IC50: 63 nM |
+
CDK6/CyclinD3, IC50: 396 nM |
+
CDK7/CyclinH, IC50: 2.87 μM |
+++
CDK9/CyclinT1, IC50: 20 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||
LDC000067 |
+
CDK2, IC50: 2.441 μM |
++
CDK9, IC50: 44 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Flavopiridol |
+++
CDK1, IC50: 40 nM |
+++
CDK2, IC50: 40 nM |
+++
CDK4, IC50: 40 nM |
+++
CDK6, IC50: 40 nM |
+
CDK7, IC50: 300 nM |
+++
CDK9, IC50: 20 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||
LY2857785 |
+
CDK7, IC50: 0.246 μM |
+++
CDK8, IC50: 0.016 μM |
+++
CDK9, IC50: 0.011 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
AZD-5438 |
+++
CDK1, IC50: 16 nM |
++++
CDK2, IC50: 6 nM |
+++
CDK9, IC50: 20 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
ML167 |
++
Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
(E/Z)-TG003 |
+++
mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
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。 |
描述 | Inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively). Abrogates G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition. Potentiates cytotoxicity of DNA-damaging drugs, enhancing the efficacy of some chemotherapeutics. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.54mL 0.51mL 0.25mL |
12.71mL 2.54mL 1.27mL |
25.42mL 5.08mL 2.54mL |
CAS号 | 135897-06-2 |
分子式 | C24H15N3O3 |
分子量 | 393.394 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 | |
动物实验配方 |