2. Stem Cell/Wnt
  3. Wnt 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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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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.
Appearance

Solid

Color

White to off-white

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (69.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7980 mL 13.9899 mL 27.9799 mL
5 mM 0.5596 mL 2.7980 mL 5.5960 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7980 mL 13.9899 mL 27.9799 mL 69.9496 mL
5 mM 0.5596 mL 2.7980 mL 5.5960 mL 13.9899 mL
10 mM 0.2798 mL 1.3990 mL 2.7980 mL 6.9950 mL
15 mM 0.1865 mL 0.9327 mL 1.8653 mL 4.6633 mL
20 mM 0.1399 mL 0.6995 mL 1.3990 mL 3.4975 mL
25 mM 0.1119 mL 0.5596 mL 1.1192 mL 2.7980 mL
30 mM 0.0933 mL 0.4663 mL 0.9327 mL 2.3317 mL
40 mM 0.0699 mL 0.3497 mL 0.6995 mL 1.7487 mL
50 mM 0.0560 mL 0.2798 mL 0.5596 mL 1.3990 mL
60 mM 0.0466 mL 0.2332 mL 0.4663 mL 1.1658 mL
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CGK012 Related Classifications

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-012Wntβ-cateninBeta cateninmultiple myelomaHUVECsHEK293-FL reporterRPMI-8226Inhibitorinhibitorinhibit

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