2. Stem Cell/Wnt
  3. β-catenin
  4. CGK012

CKG012 is an inhibitor for Wnt/βcatenin signaling pathway. CGK012 inhibits release of HMGB1 and transcription of β-catenin, exhibits attenuating activities against cecal ligation and puncture (CLP)-induced sepsis and multiple myeloma cancer.

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CGK012 Chemical Structure

CGK012 Chemical Structure

CAS No. : 2044497-76-7

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CGK012 Related Antibodies

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Description

CKG012 is an inhibitor for Wnt/βcatenin signaling pathway. CGK012 inhibits release of HMGB1 and transcription of β-catenin, exhibits attenuating activities against cecal ligation and puncture (CLP)-induced sepsis and multiple myeloma cancer[1][2].

In Vitro

CGK012 (0-20 μM) inhibits HMGB1-release by reducing LPS-induced HMGB1 acetylation and SIRT1 expression and suppresses therefore the excessive vascular permeability in HUVECs, decreases the expression of pathogen-associated molecules like TLR2/4 without affecting cellular viability of HUVECs.[1].
CGK012 (0-20 μM) exhibits ameliorates inflammatory response through decreases adhesion and migration of inflammatory immune cells, production of proinflammatory cytokines like IL-6, TNF-α, β, and transcription factors NF-kB and ERK1/2[1].
CGK012 (0-20 μM) promotes β-catenin phosphorylation/degradation and repressed the expression β-catenin-dependent genes, thereby inhibiting the proliferation of multiple myeloma cells RPMI-8226 with an IC50 of 5.08 μM[2].

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

CGK012 Related Antibodies

Cell Viability Assay[1]

Cell Line: HUVEC
Concentration: 5-100 μM
Incubation Time: 48 h
Result: Revealed no effects on cell viability.

Western Blot Analysis[1]

Cell Line: HUVECs, HEK293-FL reporter, RPMI-8226
Concentration: 0-20 μM
Incubation Time: 12 h
Result: Reduced levels of SIRT1 and acetylation of HMGB1, inhibited vascular permeability in HUVECs. Reduced levels of β-catenin in HEK293-FL reporter and RPMI-8226.

Cell Migration Assay [1]

Cell Line: HUVEC
Concentration: 0-20 μM
Incubation Time: 6 h
Result: Inhibited migration of neutrophils through monolayers of HUVECs.
In Vivo

CGK012 (0.05-0.53 mg/kg, i.v., double doses) inhibits HMGB1 release and immune cell migration, improves vascular cell stability and survival rates of C57BL/6 mice with CLP-induced sepsis[1].

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

Animal Model: CLP- induced sepsis in C57BL/6 mice[1]
Dosage: 0.26-0.53 mg/kg
Administration: double doses, 12 or 50 h after surgery.
Result: Reduced expression of HMGB1 and improved the survival rate.
Molecular Weight

357.40

Formula

C20H23NO5
CAS No.
SMILES

O=C(O[C@H]1CC2=CC(C=CC3=O)=C(O3)C=C2OC1(C)C)NC4CCCC4
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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CGK012 Related Classifications

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Help & FAQs
  • 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:

CGK0122044497-76-7CGK 012CGK-012β-cateninBeta cateninmultiple myelomaHUVECsHEK293-FL reporterRPMI-8226Inhibitorinhibitorinhibit

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