|2-(2-氟苯氧基)-4-(1-甲基-1H-吡唑-5-基)苯甲酰胺|CsnPharm

CAS No.: 2682114-39-0

2-(2-Fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)benzamide Catalog No. CSN27582

Synonyms: RBPJ INHIBITOR-1

RIN1 is a new class of small molecule inhibitor that disrupts the interaction between NOTCH and RBPJ. It also blocked the functional interaction of RBPJ with SHARP, a scaffold protein that forms a transcriptional repressor complex with RBPJ in the absence of NOTCH signaling.

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描述NOTCH proteins are trans-membrane receptors that transduce signals from cell-bound JAGGED (JAG) and Delta-like (DLL) families of ligands to mediate cell-cell interactions in processes as diverse as fetal development, heart disease and cancer. NOTCH is cleaved by γ-secretase after activation to release an intracellular domain (NICD) that binds the transcriptional effector RBPJ. RBPJ inhibitor-1 (RIN1) is the first inhibitor of RBPJ which potently disrupts the functional interaction of RBPJ with NOTCH. RIN1 inhibited Hes1-Luciferase, NOTCH3 ICD and RBPJ-VP16-dependent Hes1-Luciferase with IC₅₀s of 0.18, 0.19, and 0.2 µM and E_maxs of 82%, 88% and 81%, respectively. RIN1 (2 µM) decreased RBPJ-VP16-dependent Hes1-Luciferase activity and caused a corresponding decrease in Luciferase reporter mRNA and endogenous RBPJ target gene expression mRNAs. RIN1 decreased cell proliferation in Jurkat, Koptk-1 and Rec-1 cancer cell lines. RIN1 (0.6 µM) decreased the number of MHC⁺ cells and increased the number of nuclei per cell, indicating that it induced the formation of multinucleated myofibers^[2].
参考文献

[1] Hurtado C, Safarova A, Smith M, Chung R, Bruyneel AAN, Gomez-Galeno J, Oswald F, Larson CJ, Cashman JR, Ruiz-Lozano P, Janiak P, Suzuki T, Mercola M. Disruption of NOTCH signaling by a small molecule inhibitor of the transcription factor RBPJ. Sci Rep. 2019 Jul 25;9(1):10811. doi: 10.1038/s41598-019-46948-5. PMID: 31346210; PMCID: PMC6658660.
[2] Hurtado C, et al. Disruption of NOTCH signaling by a small molecule inhibitor of the transcription factor RBPJ. Sci Rep. 2019 Jul 25;9(1):10811

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
- 3.2122 mL
- 16.0611 mL
- 32.1223 mL
- 5 mM
- 0.6424 mL
- 3.2122 mL
- 6.4245 mL
- 10 mM
- 0.3212 mL
- 1.6061 mL
- 3.2122 mL

技术信息

CAS号	2682114-39-0	储存条件	粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C17H14FN3O2	运输	蓝冰
分子量	311.31	别名	RBPJ INHIBITOR-1

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2-(2-Fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)benzamide Catalog No. CSN27582

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