|N-(4-(3-(((5-(二甲基氨基)-1-萘基)磺酰基)氨基)苯基)-2-噻唑基)乙酰胺|CsnPharm

CAS No.: 1609402-14-3

HA15 Catalog No. CSN19076

Synonyms: HA15

HA15 is a molecule that targets specifically BiP/GRP78/HSPA5. HA15 displays anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.

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400-920-2911

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实验方案

技术信息

生物活性

描述HA15 is a thiazole benzensulfonamide that specifically targets the endoplasmic reticulum chaperone BiP. Treatment of human melanoma cell lines with 10μM of HA15 for 6 hours decreased cell viability compared with the DMSO-treated controls. The IC50 value of HA15 for the viability of A375 cells was between 1 and 2.5μM. Treatment of A375 cells with HA15 (10μM) for 4 hours greatly induced the expression of IRE1α, ATF4, and CHOP. Also, PERK and elF2α remained phosphorylated in HA15-treated cells. HA15 at 1 – 100μM significantly inhibited the ATPase activity of BiP in a dose-dependent manner. HA15 at a concentration of 10μM increased the levels of cleaved and activated form of caspase 9, and led to the cleavage of PARP in A375 cells. In mice inoculated with A375 cells, administration of HA15 (0.7mg/day) for 2 weeks markedly suppressed tumor growth without inducing hepatic toxicity.^[2]
作用机制HA15 induced a dissociation between the BiP, PERK, IRE1α, and ATF6 complex. It inhibits the activity of BiP activity by directly binding to it. HA15 inhibits tumor growth in vivo through ER stress-induced autophagy and apoptosis.^[2]
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02335164	Influenza	Phase 1	Active, not recruiting	November 1, 2018	Australia, South Australia ... more >> Flinders University Adelaide, South Australia, Australia, 5042 Collapse <<
NCT01333462	Healthy Adult Volunteers	Phase 1	Completed	-	United States, Kansas ... more >> Johnson County Clin-Trials Lenexa, Kansas, United States, 66219 Collapse <<

参考文献

[1] Cerezo M, Lehraiki A, et al. Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance. Cancer Cell. 2016 Jun 13;29(6):805-819.
[2] Cerezo M, Lehraiki A, Millet A, Rouaud F, Plaisant M, Jaune E, Botton T, Ronco C, Abbe P, Amdouni H, Passeron T, Hofman V, Mograbi B, Dabert-Gay AS, Debayle D, Alcor D, Rabhi N, Annicotte JS, Héliot L, Gonzalez-Pisfil M, Robert C, Moréra S, Vigouroux A, Gual P, Ali MMU, Bertolotto C, Hofman P, Ballotti R, Benhida R, Rocchi S. Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance. Cancer Cell. 2016 Jun 13;29(6):805-819. doi: 10.1016/j.ccell.2016.04.013. Epub 2016 May 26. Erratum in: Cancer Cell. 2016 Jul 11;30(1):183

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1433 mL
- 10.7164 mL
- 21.4327 mL
- 5 mM
- 0.4287 mL
- 2.1433 mL
- 4.2865 mL
- 10 mM
- 0.2143 mL
- 1.0716 mL
- 2.1433 mL

技术信息

CAS号

1609402-14-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H22N4O3S2

运输

蓝冰

分子量

466.58

别名

HA15

溶解度

DMSO	300.0 mg/mL (643.0 mM)
Water	insoluble

动物实验配方

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