XRP44X Bioactivity,Chemical Properties,Storage & Solubility Information Pathways-PeptideDB

Description	XRP44X (XRP 44X) is a potent inhibitor of Ras-Net (Elk-3) pathway.
In vitro	XRP44X is an indirect inhibitor of Net phosphorylation that acts upstream from Erk-1/2 activation. XRP44X inhibits luciferase activity with the IC50 of～10 nM[1].XRP44X (10 nM) inhibits cell growth of HUVEC, NIH3T3, HCT-116, and NIH3T3–Ki-Ras cells[1].XRP44X (100 nM) inhibits phosphorylation of Mek-1/2 and Raf-1[1].
In vivo	XRP44X具有治疗难治性哮喘的潜力[1]。作为Ras/Erk激活转录因子Elk3的抑制剂，XRP44X在裸鼠中抑制肿瘤生长和转移。通过抑制肿瘤生长及裸鼠中的转移形成，XRP44X显示了其对抗肿瘤及转移的潜在效用[2]。
Target activity	Ras:10 nM
Synonyms	XRP-44-X, XRP 44X, XRP-44X, XRP 44 X
molecular weight	380.87
Molecular formula	C21H21ClN4O
CAS	729605-21-4
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
Solubility	DMSO: 36.67 mg/ml (96.27 mM)
References	1. Li TZ, Kim SM, Hur W, Choi JE, Kim JH, Hong SW, Lee EB, Lee JH, Yoon SK. Elk-3 Contributes to the Progression of Liver Fibrosis by Regulating the Epithelial-Mesenchymal Transition. Gut Liver. 2017 Jan 15;11(1):102-111. doi: 10.5009/gnl15566. PubMed PMID: 27538444; PubMed Central PMCID: PMC5221867. 2. Semenchenko K, Wasylyk C, Cheung H, Tourrette Y, Maas P, Schalken JA, van der Pluijm G, Wasylyk B. XRP44X, an Inhibitor of Ras/Erk Activation of the Transcription Factor Elk3, Inhibits Tumour Growth and Metastasis in Mice. PLoS One. 2016 Jul 18;11(7):e0159531. doi: 10.1371/journal.pone.0159531. eCollection 2016. PubMed PMID: 27427904; PubMed Central PMCID: PMC4948895. 3. Chen J, Sun WL, Wasylyk B, Wang YP, Zheng H. c-Jun N-terminal kinase mediates microtubule-depolymerizing agent-induced microtubule depolymerization and G2/M arrest in MCF-7 breast cancer cells. Anticancer Drugs. 2012 Jan;23(1):98-107. doi: 10.1097/CAD.0b013e32834bc978. PubMed PMID: 21968419. 4. Wasylyk C, Zheng H, Castell C, Debussche L, Multon MC, Wasylyk B. Inhibition of the Ras-Net (Elk-3) pathway by a novel pyrazole that affects microtubules. Cancer Res. 2008 Mar 1;68(5):1275-83. doi: 10.1158/0008-5472.CAN-07-2674. PubMed PMID: 18316589.

PeptideDB

XRP44X

CAS No.: 729605-21-4