[CAS NO. 2673364-10-6] DDO3711
PRODUCTS SPECIFICATIONS [2673364-10-6]
DESCRIPTION [2673364-10-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 767.83 |
| Molecular Formula | C42H41N9O6 |
| SMILES | COC1=CC=C(C=C1OC)C2=NC(CC3=CC=C(C=C3)C(NCCCCCCNC(C4=CC=C(C=C4)C(NC5=CN6C=C(C=CC6=N5)N7C=CN=C7)=O)=O)=O)=NO2 |
Summary
DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 ( IC 50 =164.1 nM) not ASK2 (IC 50 >20 μM). DDO3711 significantly dephosphorylates p-ASK1 T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research [1] .
IC50 & Target
|
ASK1 164.1 nM (IC 50 ) |
ASK2 >20 μM (IC 50 ) |
In Vitro
DDO3711 (15 μM; 24 h) shows antiproliferation effects on gastric cancer cells by reducing p-ASK1
T838
in a PP5-dependent manner. DDO3711 does not inhibit the proliferation of GES-1 cells and HGC-27 cells
[1]
.
DDO3711 (5 μM; 1-24 h) inhibited the expression of CDK4/6 and cyclin D1 in a concentration-dependent manner
[1]
.
DDO3711 (5-50 μM; 0.5-2 h) potently dephosphorylates p-ASK1
T838
both in vitro and in cells. DDO3711 concentration-dependently reduced the level of p-JNK and p-p38
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [1]
| Cell Line: | MKN45 cells |
| Concentration: | 15 μM |
| Incubation Time: | 24 h |
| Result: | Showed strong antiproliferative activity (IC 50 =0.5 μM). |
Cell Cycle Analysis [1]
| Cell Line: | MKN45 cells |
| Concentration: | 5 μM |
| Incubation Time: | 1-24 h |
| Result: | Inhibited the expression of CDK4/6 and cyclin D1 in a concentration-dependent manner. |
Western Blot Analysis [1]
| Cell Line: | MKN45 cells |
| Concentration: | 5, 25, 50 μM |
| Incubation Time: | 0.5-2 h |
| Result: | Could dephosphorylate p-ASK1 T838 in a time- and concentration-dependent manner in vitro. |
In Vivo
DDO3711 (20, 40 mg/kg; IP; daily; for 21 days) causes significant inhibition of tumor growth in a dose-dependent manner
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Four-week-old BALB/c nude mice with MKN45 cells [1] |
| Dosage: | 20, 40 mg/kg |
| Administration: | IP; daily; for 21 days |
| Result: |
Caused significant inhibition of tumor growth in a dose-dependent manner.
Significantly decreased the level of p-ASK1 T838 . |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.