2. Apoptosis Cell Cycle/DNA Damage Metabolic Enzyme/Protease Immunology/Inflammation NF-κB MAPK/ERK Pathway Stem Cell/Wnt
  3. MDM-2/p53 CDK Caspase Bcl-2 Family Reactive Oxygen Species p38 MAPK ERK JNK
  4. MAPK-IN-3

MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK.

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MAPK-IN-3 Chemical Structure

MAPK-IN-3 Chemical Structure

CAS No. : 2848599-79-9

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MAPK-IN-3 Related Antibodies

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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ERK ERK1 ERK2 ERK5 ERK8

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JNK1 JNK2 JNK3 JNK

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Description

MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK[1].

IC50 & Target

Cyclin D1

 

Cyclin B1

 

Caspase 9

 

Caspase-7

 

Molecular Weight

556.56

Formula

C28H32N2O10
CAS No.
SMILES

COC1=C(C=C2OC3=C(C(O)=C(C(OCC(NO)=O)=C3)C/C=C(C)\C)C(C2=C1C/C=C(C)\C)=O)OCC(NO)=O
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Purity & Documentation
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MAPK-IN-3 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:

MAPK-IN-32848599-79-9MDM-2/p53CDKCaspaseBcl-2 FamilyReactive Oxygen Speciesp38 MAPKERKJNKCyclin dependent kinaseExtracellular signal regulated kinasesc-Jun N-terminal kinaseKYSE 30HCT 116HGC 27Antiproliferative AgentsInhibitorinhibitorinhibit

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