HS-243

立即咨询

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。

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-4和IRAK-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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 mg

5 mg

10 mg

1 mM	3.0833 mL	15.4164 mL	30.8328 mL
5 mM	0.6167 mL	3.0833 mL	6.1666 mL
10 mM	0.3083 mL	1.5416 mL	3.0833 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。