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HS-243
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HS-243图片
CAS NO:848249-10-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
HS-243 是一种有效且选择性的IRAK-4IRAK-1抑制剂,IC50为 20 和 24 nM。HS-243 对TAK1(转化生长因子 β 活化激酶 1) 有微弱的抑制活性,IC50为 0.5 μM。HS-243 具有抗炎和抗癌活性。
生物活性

HS-243 is a potent and selectiveIRAK-4andIRAK-1inhibitor, withIC50values of 20 and 24 nM. HS-243 shows minimalTAK1(transforming growth factor β-activated kinase 1) inhibition activity, with aIC50of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity[1].

IC50& Target

IRAK4

20 nM (IC50)

IRAK-1

24 nM (IC50)

CLK4

662 nM (IC50)

体外研究
(In Vitro)

HS-243 (0-10 μM, 24 h) inhibits cell survival by 21% for AN3-CA (pancreatic cancer cell), and 13% for SKOV-3 (ovarian cancer cell)[1].
HS-243 (10 μM, 24 h) potently reduces the proinflammatory response of RA cells and macrophages, significantly reduces 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 shows minimal to no percentage of inhibition against IRAK-4 Y262T or Y262A mutants at 0.3 and 1 μM[1].

Cell Viability Assay[1]

Cell Line:SK-OV-3, AN3-CA, H460, ES-2, SK-UT-1B, COLO205, Bx-PC-3
Concentration:1 nM, 10 nM, 100 nM, 1 μM, 10 μM, and 10 μM+IL-1β (30 ng/ml)
Incubation Time:24 h
Result:Inhibited cell survival by 21% for AN3-CA (pancreatic), and 13% for SKOV-3 (ovarian). The addition of IL-1β in conjunction with HS-243 increased cell death to 46% in SK-OV-3 (ovarian), 33% in AN3-CA (pancreatic), and 31% in H460 (colon).
分子量

324.33

性状

Solid

Formula

C17H16N4O3

CAS 号

848249-10-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 41.67 mg/mL(128.48 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.0833 mL15.4164 mL30.8328 mL
5 mM0.6167 mL3.0833 mL6.1666 mL
10 mM0.3083 mL1.5416 mL3.0833 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。