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首页-抗体药物偶连体和PROTACs-PROTAC-RNK06138
RNK06138

Chemical Structure : RNK06138

CAS No.: 2768085-98-7

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RNK06138 (RNK-06138)

货号: PC-28724Not For Human Use, Lab Use Only.

RNK06138 is a potent, tumor-selective, and efficacious chaperone-mediated ERK5 degrader (Chaperone-Mediated Protein Degradation, CHAMP), binds HSP90 with IC50 of 306 nM, inhibits ERK5 kinase activity with IC50 of 615 nM, decreases ERK5 protein levels with Dmax of 74% and DC50 of 111.7 nM in MOLP-8 myeloma cell line.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

RNK06138 is a potent, tumor-selective, and efficacious chaperone-mediated ERK5 degrader (Chaperone-Mediated Protein Degradation, CHAMP), binds HSP90 with IC50 of 306 nM, inhibits ERK5 kinase activity with IC50 of 615 nM, decreases ERK5 protein levels with Dmax of 74% and DC50 of 111.7 nM in MOLP-8 myeloma cell line.
RNK06138 shows no off-target kinase inhibition at the concentration 1 uM.
RNK06138 can degrade endogenous ERK5 protein in a panel of tumor cell lines.
RNK06138 induces ERK5 degradation via a UPS-mediated mechanism.
RNK06138 reduces nuclear ERK5 and attenuates ERK5 Paradoxical activation.
RNK06138 hampers the nuclear localization of ERK5 and the subsequent transcriptional activation of downstream targets.
RNK06138 inhibits cell growth in various cancer cell lines (IC50=98.39 nM), inhibits cell proliferation and induces apoptosis.
RNK06138 shows tumor-targeted pharmacokinetics and anti-tumor potency.

物理化学性质&存储条件

分子量 1164.32
分子式 C58H68F3N13O8S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-(4-((4-((1-(1-(3-ethoxy-4-((5-methyl-11-(methylsulfonyl)-6-oxo-6,11-dihydro-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-2-yl)amino)phenyl)piperidine-4-carbonyl)piperidin-4-yl)methyl)piperazin-1-yl)methyl)phenyl)-5-(5-ethyl-2,4-dihydroxyphenyl)-N-(1,1,1-trifluoropropan-2-yl)-4H-1,2,4-triazole-3-carboxamide

参考文献

1. Xiangcai Yang, et al. Cell Commun Signal. 2026 Feb 3;24(1):157.

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