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MedChemExpress - Model Cysmethynil - ...

MedChemExpress - Model Cysmethynil - 851636-83-4

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].

Cysmethynil

MCE China：Cysmethynil

Brand：MedChemExpress (MCE)

Cat. No.HY-16160

CAS：851636-83-4

Purity：99.87%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：Cysmethynil (15 μM or 20 μM or 30 μM; 6 days) inhibits Icmt+/+ cells and Icmt-/-/ICMT cells proliferation, unaffects Icmt-/-cells growth [1]. Cysmethynil (20-30 μM; 1-6 days) inhibits PC3 cells proliferation and results in a dose- and time-dependent reduction in the number of viable PC3 cells[2].

In Vivo：Cysmethynil (100 mg/kg, 200 mg/kg; intraperitoneal injection; every 48 h; 28 day) without adverse effects on mice body weight, significantly impacts on tumor growth, causes both an accumulation of cells in the G1 phase and cell death [2]. Cysmethynil (20 mg/kg; intraperitoneal injection; three times a week; 2 weeks; alone or combined with Paclitaxel (HY-B0015)/ Doxorubicin (HY-15142A) ) is not toxic to mice and induces only moderate inhibition of tumor growth as single agent, the combination with Paclitaxel(HY-B0015)/ Doxorubicin(HY-15142A) results in significantly greater efficacy in inhibiting tumor growth. Cysmethynil sensitizes cervical cancer cells to chemotherapy agent in xenograft mouse model[3].

IC50 & Target：IC50 = 2.4 μM for Icmt Cellular Effect Cell Line Type Value Description References

References：

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[4]. Zhu C, et al. Targeting KRAS mutant cancers: from druggable therapy to drug resistance. Mol Cancer. 2022 Aug 4;21(1):159. [Content Brief]

Brand introduction:
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