HS-243

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。

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
5mg

￥1300.00

1040.00

- +
10mg

￥2287.00

1830.00

- +
25mg

￥3887.00

3110.00

- +
50mg

￥6262.00

5010.00

- +
100mg

￥9387.00

7510.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajcf18626
CAS: 848249-10-5
别名:
分子式: C17H16N4O3
分子量: 324.33
纯度: >98%
溶解度: DMSO : 41.67 mg/mL (128.48 mM; Need ultrasonic)
储存: Store at -20°C
库存: 现货

Background

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

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).

[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.