SB-218078 | Chk1 Inhibitor | AmBeed-信号通路专用抑制剂

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SB-218078 {[allProObj[0].p_purity_real_show]}

货号：A465968

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.

SB-218078 化学结构
CAS号：135897-06-2

SB-218078 3D分子结构
CAS号：135897-06-2

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SB-218078 纯度/质量文件产品仅供科研

货号：A465968 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

PKC 亚型比较
转化生长因子-β 亚型比较
Chk 亚型比较
CDK 亚型比较

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 ↓ ↑	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。

SB-218078 生物活性

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.

SB-218078 实验方案

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

SB-218078 技术信息

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

SB-218078 {[allProObj[0].p_purity_real_show]}

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