HS-243

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

HS-243 是 IRAK-4 和 IRAK-1 的抑制剂，IC50 分别为 20 和 24 nM。 HS-243 显示出抗炎和抗癌活性。

HS-243 is an inhibitor of IRAK-4 and IRAK-1 with IC50s of 20 and 24 nM. HS-243 shows anti-inflammatory and anticancer activity.(In Vitro):HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 (0-10 μM) inhibits cell survival by 21% for AN3-CA pancreatic cancer cells, and 13% for SKOV-3 ovarian cancer cells. HS-243 (10 μM) potently reduces the pro-inflammatory response of RA cells and macrophages and 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.

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).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. HS-243 shows minimal to no percentage of inhibition against IRAK-4 Y262T or Y262A mutants at 0.3 and 1 μM. Cell Viability Assay 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).

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Immunology/Inflammation

IRAK

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848249-10-5

324.34

C17H16N4O3

>98% (HPLC)

In Vitro:?DMSO : 41.67 mg/mL (128.48 mM)

CCCn1c(NC(=O)c2cccc(c2)[N+]([O-])=O)nc2ccccc12

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(-20℃)

With Ice Pack

≥ 2 years