2. MAPK/ERK Pathway
  3. MAP3K
  4. DDO3711

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 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research.

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DDO3711 Chemical Structure

DDO3711 Chemical Structure

CAS No. : 2673364-10-6

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DDO3711 Related Antibodies

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Description

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 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1T838 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[1]

ASK1

164.1 nM (IC50)

ASK2

>20 μM (IC50)

In Vitro

DDO3711 (15 μM; 24 h) shows antiproliferation effects on gastric cancer cells by reducing p-ASK1T838 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-ASK1T838 both in vitro and in cells. DDO3711 concentration-dependently reduced the level of p-JNK and p-p38[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DDO3711 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MKN45 cells
Concentration: 15 μM
Incubation Time: 24 h
Result: Showed strong antiproliferative activity (IC50=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-ASK1T838 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].

MedChemExpress (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-ASK1T838.
Molecular Weight

767.83

Formula

C42H41N9O6
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DDO3711 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DDO37112673364-10-6DDO 3711DDO-3711MAP3KMAP kinase kinase kinase, MEKK, MAPKKKPP5phosphatase recruitment chimerasPHORCsapoptosis signal-regulated kinase 1ASK1ASK2p-ASK1T838 abnormally phosphorylated oncoproteinsMKN45Inhibitorinhibitorinhibit

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