Cysmethynil
Based on 1 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.07%
- CAS. Nr.: 851636-83-4
- Formel: C25H32N2O
- Molecular Weight:376.53
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Cysmethynil
More
Biologische Aktivität
IC50 = 2.4 μM for Icmt
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
19.3 μM
Compound: 1
|
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
|
[PMID: 23514631] |
| IMR-90 | IC50 |
29.2 μM
Compound: 1
|
Antiproliferative activity against human IMR90 cells after 72 hrs by MTT assay
Antiproliferative activity against human IMR90 cells after 72 hrs by MTT assay
|
[PMID: 23514631] |
| MDA-MB-231 | IC50 |
21.8 μM
Compound: 45292
|
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by colorimetric tetrazolium assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by colorimetric tetrazolium assay
|
[PMID: 20809634] |
| MDA-MB-231 | IC50 |
22.1 μM
Compound: 1
|
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
|
[PMID: 23514631] |
| PC-3 | IC50 |
21.3 μM
Compound: 1
|
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
|
[PMID: 23514631] |
| Sf9 | IC50 |
1.5 μM
Compound: 45292
|
Inhibition of recombinant ICMT expressed in Sf9 cells using [3H] AdoMet after 20 mins by scintillation counting
Inhibition of recombinant ICMT expressed in Sf9 cells using [3H] AdoMet after 20 mins by scintillation counting
|
[PMID: 20809634] |
| Sf9 | IC50 |
2.4 μM
Compound: cysmethynil
|
Inhibition of recombinant ICMT expressed in Sf9 cells using [3H]-AdoMet after 20 mins by scintillation counter
Inhibition of recombinant ICMT expressed in Sf9 cells using [3H]-AdoMet after 20 mins by scintillation counter
|
[PMID: 21661760] |
| Sf9 | IC50 |
1.9 μM
Compound: 1
|
Inhibition of recombinant Icmt (unknown origin) expressed in Sf9 cells assessed as transfer of methyl group from [3H]-S-adenosylmethionine to [3H]-biotin-S-farnesyl-L-cysteine after 30 mins
Inhibition of recombinant Icmt (unknown origin) expressed in Sf9 cells assessed as transfer of methyl group from [3H]-S-adenosylmethionine to [3H]-biotin-S-farnesyl-L-cysteine after 30 mins
|
[PMID: 23514631] |
| Sf9 | IC50 |
2.4 μM
Compound: 31
|
Inhibition of recombinant ICMT (unknown origin) expressed in sf9 cells using biotin S-farnesyl-L-cysteine as substrate
Inhibition of recombinant ICMT (unknown origin) expressed in sf9 cells using biotin S-farnesyl-L-cysteine as substrate
|
[PMID: 23566315] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:PC3 cells[2]
-
Concentration:20-30 μM cysmethynil
-
Incubation Time:1-6 days
-
Result:Resulted in a dose- and time-dependent reduction in the number of viable PC3 cells.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:6 week-old SCID mice with SiHa cells in the mice flank [3]
-
Dosage:20 mg/kg (single; combination with Paclitaxel or Doxorubicin)
-
Administration:intraperitoneal injection; three times a week; 2 weeks
-
Result:Decreased in tumor size when treated with Cys alone, or Cysmethynil+Paclitaxel(HY-B0015)/Cysmethynil+ Doxorubicin(HY-15142A) .
-
Animal Model:SCID mice with PC3 cells in a xenograft model[2]
-
Dosage:0.1 mg/g or 0.2 mg/g Cysmethynil
-
Administration:intraperitoneal injection; every 48 h; 28 days
-
Result:Decreased in tumor size when treated with both doses of cysmethynil.
Chemical Information
-
CAS. Nr. 851636-83-4
-
Appearance Solid
-
Molecular Weight 376.53
-
Formel C25H32N2O
-
Color White to light yellow
-
SMILES
O=C(N)CC1=CN(CCCCCCCC)C2=C1C=C(C3=CC=CC(C)=C3)C=C2
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
J Ovarian Res
Vitamin B6 promotes the activation of primordial follicles through the PI3K/Akt signaling pathway. [Abstract]2025 Dec 17;18(1):296. PMID: 41408298
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (265.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
-
Data Sheet (276 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
Verweise
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6558 mL | 13.2792 mL | 26.5583 mL | 66.3958 mL |
| 5 mM | 0.5312 mL | 2.6558 mL | 5.3117 mL | 13.2792 mL | |
| 10 mM | 0.2656 mL | 1.3279 mL | 2.6558 mL | 6.6396 mL | |
| 15 mM | 0.1771 mL | 0.8853 mL | 1.7706 mL | 4.4264 mL | |
| 20 mM | 0.1328 mL | 0.6640 mL | 1.3279 mL | 3.3198 mL | |
| 25 mM | 0.1062 mL | 0.5312 mL | 1.0623 mL | 2.6558 mL | |
| 30 mM | 0.0885 mL | 0.4426 mL | 0.8853 mL | 2.2132 mL | |
| 40 mM | 0.0664 mL | 0.3320 mL | 0.6640 mL | 1.6599 mL | |
| 50 mM | 0.0531 mL | 0.2656 mL | 0.5312 mL | 1.3279 mL | |
| 60 mM | 0.0443 mL | 0.2213 mL | 0.4426 mL | 1.1066 mL | |
| 80 mM | 0.0332 mL | 0.1660 mL | 0.3320 mL | 0.8299 mL | |
| 100 mM | 0.0266 mL | 0.1328 mL | 0.2656 mL | 0.6640 mL |