Cysmethynil

CAS: 851636-83-4 F: C25H32N2O W: 376.53

Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction

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Bioactivity	Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research[1][2][3].
Target	IC50 = 2.4 μM for Icmt
Invitro	Cysmethynil (15 μM or 20 μM or 30 μM; 6天) 抑制 Icmt+/+ 细胞和 Icmt-/- /ICMT 细胞增殖，不影响 Icmt-/- 细胞生长[1]。Cysmethynil (20-30 μM; 1-6 天) 抑制 PC3 细胞增殖，导致存活 PC3 细胞数量呈剂量和时间依赖性减少[2]。 0 --> Cysmethynil 相关抗体: Cell Viability Assay Cell Line:
In Vivo	Cysmethynil（100 mg/kg, 200 mg/kg; 腹腔注射;每48小时一次;28天）对小鼠体重无不良影响，会显着影响肿瘤生长，导致 G1 期细胞积聚和细胞死亡[2]。Cysmethynil（20 mg/kg; 腹腔注射;每周3次;2周;单独使用或与 Paclitaxel (HY-B0015)/ Doxorubicin (HY-15142A) 联用）对小鼠无毒性，并且作为单药诱导仅中度抑制肿瘤生长，与 Paclitaxel (HY-B0015)/ Doxorubicin (HY-15142A) 联用可显着提高治疗效果，抑制肿瘤生长。Cysmethynil 在异种移植小鼠模型中使宫颈癌细胞对化疗药物敏感[3]。 Animal Model:
Name	Cysmethynil
CAS	851636-83-4
Formula	C25H32N2O
Molar Mass	376.53
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Winter-Vann AM, et al. A small-molecule inhibitor of isoprenylcysteine carboxyl methyltransferase with antitumor activity in cancer cells. Proc Natl Acad Sci U S A. 2005 Mar 22;102(12):4336-41. [2]. Wang M, et al. A small molecule inhibitor of isoprenylcysteine carboxymethyltransferase induces autophagic cell death in PC3 prostate cancer cells. J Biol Chem. 2008 Jul 4;283(27):18678-84. [3]. Pan Q, et al. Inhibition of isoprenylcysteine carboxylmethyltransferase sensitizes common chemotherapies in cervical cancer via Ras-dependent pathway. Biomed Pharmacother. 2018 Mar;99:169-175. [4]. Zhu C, et al. Targeting KRAS mutant cancers: from druggable therapy to drug resistance. Mol Cancer. 2022 Aug 4;21(1):159.