3MB-PP1 | Purine Analog | AmBeed-信号通路专用抑制剂

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3MB-PP1 {[allProObj[0].p_purity_real_show]}

货号：A247643

3MB-PP1是一种嘌呤类似物，是一种 Polo 样激酶 1 (Plk1) 抑制剂。靶向突变的 Plk1 等位基因，阻断细胞有丝分裂。其特异性抑制 Cdk8 及 ZIPK 激酶的活性，常用于研究细胞分裂和白色念珠菌感染的机制。

3MB-PP1 化学结构
CAS号：956025-83-5

3MB-PP1 3D分子结构
CAS号：956025-83-5

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3MB-PP1 纯度/质量文件产品仅供科研

货号：A247643 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 >

CDK 亚型比较
PLK 亚型比较

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											SGK,ERK	{[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/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 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/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 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												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		{[allProObj[0].p_purity_real_show]}
(E/Z)-TG003												+++ mCLK4, IC50: 15 nM mCLK1, IC50: 200 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	PLK1 ↓ ↑	PLK2 ↓ ↑	PLK3 ↓ ↑	PLK4 ↓ ↑	其他靶点	纯度
HMN-214	✔					{[allProObj[0].p_purity_real_show]}
SBE13 HCl	++++ PLK1, IC50: 200 pM					{[allProObj[0].p_purity_real_show]}
Onvansertib	+++ PLK1, IC50: 2 nM					{[allProObj[0].p_purity_real_show]}
Volasertib	++++ PLK1, IC50: 0.87 nM					{[allProObj[0].p_purity_real_show]}
GSK461364	+++ PLK1, Ki: 2.2 nM					{[allProObj[0].p_purity_real_show]}
MLN0905	+++ PLK1, IC50: 2 nM					{[allProObj[0].p_purity_real_show]}
Ro3280	++ PLK1, IC50: 3 nM					{[allProObj[0].p_purity_real_show]}
(E/Z)-Rigosertib sodium	+ PLK1, IC50: 9 nM	+ PLK2, IC50: 260 nM			Bcr-Abl	{[allProObj[0].p_purity_real_show]}
BI 2536	++++ PLK1, IC50: 0.83 nM	++ PLK2, IC50: 3.5 nM	+ PLK3, IC50: 9.0 nM			{[allProObj[0].p_purity_real_show]}
CFI-400945				++ PLK4, IC50: 2.8 nM	Tie-2	{[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。

3MB-PP1 生物活性

描述

3MB-PP1 is a bulky purine analog and a PLK1 inhibitor. In cells expressing an analogue-sensitive Plk1 allele, 3MB-PP1 blocks mitotic progression and cytokinesis by targeting PLK1. 3MB-PP1 specifically inhibits analogue-sensitive Cdk8 activity. 3MB-PP1 inhibits Leu93-ZIPK with an IC50 value of 2 μM. 3MB-PP1 can be used to study Candida albicans mycelium formation and cell division^[1]^[2]^[3].3-MB-PP1 at 5μM stimulates hyphal growth in a strain bearing analog-sensitive alleles of CDK8, post 3-hour treatment at 30℃^[2].

3MB-PP1 参考文献

[1]Burkard ME, et al. Enabling and disabling polo-like kinase 1 inhibition through chemical genetics. ACS Chem Biol. 2012 Jun 15;7(6):978-81.

[2]Hollomon JM, et al. The Candida albicans Cdk8-dependent phosphoproteome reveals repression of hyphal growth through a Flo8-dependent pathway. PLoS Genet. 2022;18(1):e1009622. Published 2022 Jan 4.

[3]Al-Ghabkari A, et al. Validation of chemical genetics for the study of zipper-interacting protein kinase signaling. Proteins. 2018 Nov;86(11):1211-1217.

3MB-PP1 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.39mL

0.68mL

0.34mL

16.93mL

3.39mL

1.69mL

33.85mL

6.77mL

3.39mL

3MB-PP1 技术信息

CAS号	956025-83-5
分子式	C₁₇H₂₁N₅
分子量	295.382

别名
运输	蓝冰

存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(355.47 mM)，配合低频超声，并水浴加热至45℃助溶，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

3MB-PP1 {[allProObj[0].p_purity_real_show]}

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