SC-43
SC-43 Basic information
- Product Name:
- SC-43
- Synonyms:
-
- 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(3-(4-cyanophenoxy)phenyl)urea
- SC-43
- Urea, N-[4-chloro-3-(trifluoromethyl)phenyl]-N'-[3-(4-cyanophenoxy)phenyl]-
- antiproliferative,Inhibitor,SC-43,SHP-1,PTPN6,Phosphatase,Apoptosis,caspase-3,SC 43,anti-fibrotic,p-STAT3,anticancer,orally,SC43,PARP,STAT,inhibit
- SC-43, 10 mM in DMSO
- SC-43 ，S0445
- CAS:
- 1400989-25-4
- MF:
- C21H13ClF3N3O2
- MW:
- 431.8
- Mol File:
- 1400989-25-4.mol
SC-43 Chemical Properties
- Boiling point:
- 462.0±45.0 °C(Predicted)
- Density
- 1.46±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 250 mg/mL (578.97 mM)
- form
- A solid
- pka
- 12.92±0.70(Predicted)
- color
- White to off-white
- InChI
- InChI=1S/C21H13ClF3N3O2/c22-19-9-6-15(11-18(19)21(23,24)25)28-20(29)27-14-2-1-3-17(10-14)30-16-7-4-13(12-26)5-8-16/h1-11H,(H2,27,28,29)
- InChIKey
- QIBWSQJZKMUZAK-UHFFFAOYSA-N
- SMILES
- N(C1=CC=C(Cl)C(C(F)(F)F)=C1)C(NC1=CC=CC(OC2=CC=C(C#N)C=C2)=C1)=O
SC-43 Usage And Synthesis
Uses
SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects[1][2].
Biological Activity
SC-43 is a derivative of sorafenib, an agonist of Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6), which reduces liver fibrosis. SC-43 can reduce p-STAT3 and induce apoptosis, and has antitumor activity.
in vitro
SC-43 (0-10 μM; 24-72 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment reveals the anti-proliferative effects in cholangiocarcinoma (CCA) cell lines in a dose-dependent manner after treating 24, 48 and 72 hours respectively.
Its treatment shows increased sub-G1 cells and G2-M arrest, indicating SC-43 induced differential apoptotic effects in these cell lines.
Its (0-10 μM; 24 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment demonstrates significant increase in cleaved caspase-3 and PARP level.
Its activates SH2 domain-containing phosphatase 1 (SHP-1) activity, leading to p-STAT3 and downstream cyclin B1 and Cdc2 downregulation. Its augments SHP-1 activity by direct binding to N-SH2 and relief of its autoinhibition.
Cell Cycle Analysis
| Cell Line: | HuCCT-1, KKU-100, and CGCCA cells |
| Concentration: | 0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM |
| Incubation Time: | 24 hours |
| Result: | Showed increased sub-G1 cells and G2-M arrest. |
Western Blot Analysis
| Cell Line: | HuCCT-1, KKU-100, and CGCCA cells |
| Concentration: | 0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM |
| Incubation Time: | 24 hours |
| Result: | Demonstrated significant increase in cleaved caspase-3 and PARP level. |
in vivo
SC-43 (10-30 mg/kg; oral gavage; daily; for 23 days; male NCr athymic nude mice) treatment exhibits xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation.
| Animal Model: | Male NCr athymic nude mice (5-7 weeks of age) injected with HuCCT-1 cells |
| Dosage: | 10 mg/kg or 30 mg/kg |
| Administration: | Oral gavage; daily; for 23 days |
| Result: | Exhibited xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation. |
target
| Target | Value |
| SHP-1 () | |
| STAT3 () |
IC 50
SHP-1; p-STAT3
References
[1] Ming-Hung Hu, et al. Targeting SHP-1-STAT3 signaling: A promising therapeutic approach for the treatment of cholangiocarcinoma. Oncotarget. 2017 May 10;8(39):65077-65089. DOI:10.18632/oncotarget.17779
[2] Tung-Hung Su, et al. Src-homology protein tyrosine phosphatase-1 agonist, SC-43, reduces liver fibrosis. Sci Rep. 2017 May 11;7(1):1728. DOI:10.1038/s41598-017-01572-z
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