|5-[(7-氯-1H-吲哚-3-基)甲基]-3-甲基-2,4-咪唑烷二酮|CsnPharm

CAS No.: 852391-15-2

Necrostatin 2 racemate Catalog No. CSN15733

Synonyms: Necrostatin-1 stable;Necrostatin 1S;Nec-1S

Necrostatin 2 is a potent necroptosis inhibitor with EC50 of 50 nM.

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技术信息

生物活性

描述RIPK1 is a key regulator of innate immune signalling pathways. To ensure an optimal inflammatory response, RIPK1 is regulated post-translationally by well-characterized ubiquitylation and phosphorylation events, as well as by caspase-8-mediated cleavage^[3].RIPK1 and RIPK3 (receptor-interacting serine/threonine protein kinases 1/3) interact by virtue of their RIP homotypic interaction motifs to mediate a form of cell death called necroptosis, although mice lacking these kinases have very different phenotypes. RIPK1-deficient mice die soon after birth, whereas RIPK3-deficient mice are healthy. Necroptosis involves cell rupture and is triggered by tumor necrosis factor (TNF), Toll-like receptors (TLRs), or the T cell receptor (TCR) when pro-apoptotic caspase-8 is inhibited^[4]. In lesional psoriatic epidermis, RIPK1-expression was decreased compared with that in normal epidermis. Cytokines involved in the pathomechanism of psoriasis, such as IL-1β, IL-17A, IL-22 and TRAIL, reduced RIPK1-expression in normal human epidermal keratinocytes (HEK) in vitro. In addition, RIPK1-knockdown enhanced TRAIL-mediated expression of psoriasis-relating cytokines, such as IL-1β, IL-6, IL-8, TNF-α, in HEK^[5].RIPK1 is upregulated in human colorectal cancer and promotes cell proliferation when overexpressed in a colon cancer cell line. RIPK1 interacts with mitochondrial Ca2+ uniporter (MCU) to promote proliferation by increasing mitochondrial Ca2+ uptake and energy metabolism. The ubiquitination site of RIPK1 (RIPK1-K377) was critical for this interaction with MCU and function in promoting cell proliferation^[6].Necrostatin 2 racemate is an potent and specific inhibitor of RIPK1^[7].
参考文献

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
- 3.6009 mL
- 18.0046 mL
- 36.0093 mL
- 5 mM
- 0.7202 mL
- 3.6009 mL
- 7.2019 mL
- 10 mM
- 0.3601 mL
- 1.8005 mL
- 3.6009 mL

技术信息

CAS号

852391-15-2

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H12ClN3O2

运输

蓝冰

分子量

277.71

别名

Necrostatin-1 stable;Necrostatin 1S;Nec-1S;7-Cl-O-Nec1;(±)-Necrostatin-2;Necrostatin-2

溶解度

DMSO	54.0 mg/mL (194.5 mM)
Water	Insoluble
Ethanol	9.0 mg/mL (32.4 mM)

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Necrostatin 2 racemate Catalog No. CSN15733

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