HS-243 | IRAK-1/4 Inhibitor | AmBeed-信号通路专用抑制剂

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HS-243 {[allProObj[0].p_purity_real_show]}

货号：A1598756

HS-243是一种有效且选择性的IRAK-4和IRAK-1抑制剂，具有抗炎和抗癌活性，并对TAK1有微弱抑制作用，用于相关疾病研究。

HS-243 化学结构
CAS号：848249-10-5

HS-243 3D分子结构
CAS号：848249-10-5

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HS-243 纯度/质量文件产品仅供科研

货号：A1598756 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

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(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 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												++ Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 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。

HS-243 生物活性

描述

HS-243 is a potent and selective inhibitor of IRAK-4 and IRAK-1, with IC50 values of 20 nM and 24 nM, respectively. It exhibits minimal inhibition of TAK1 (transforming growth factor β-activated kinase 1), with an IC50 of 0.5 µM. HS-243 demonstrates anti-inflammatory and anticancer properties^[1].

体外研究

HS-243 (0-10 µM, 24 hours) reduces cell survival by 21% in AN3-CA (pancreatic cancer cells) and by 13% in SKOV-3 (ovarian cancer cells)^[1].

HS-243 (10 μM, 24 hours) strongly diminishes the proinflammatory response in RA cells and macrophages, significantly lowering the secretion of 15 cytokines, including IL-8, CD14, GRO-α, MIP-1a, MIP-3a, uPAR, Osteopontin, MMP-9, MCP-1, I-TAC, TIM-3, IP-10, GDF-15, and RANTES^[1].

HS-243 exhibits minimal or no inhibition against IRAK-4 Y262T or Y262A mutants at concentrations of 0.3 and 1 μM^[1].

HS-243 参考文献

[1]Scarneo SA, et al. A highly selective inhibitor of interleukin-1 receptor-associated kinases 1/4 (IRAK-1/4) delineates the distinct signaling roles of IRAK-1/4 and the TAK1 kinase. J Biol Chem. 2020 Feb 7;295(6):1565-1574.

HS-243 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.08mL

0.62mL

0.31mL

15.42mL

3.08mL

1.54mL

30.83mL

6.17mL

3.08mL

HS-243 技术信息

CAS号	848249-10-5
分子式	C₁₇H₁₆N₄O₃
分子量	324.334

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: 40 mg/mL(123.33 mM)，配合低频超声助溶，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

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