2. Others NF-κB Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. Drug Derivative NF-κB MMP TNF Receptor Interleukin Related Cyclin G-associated Kinase (GAK) CDK PI3K Akt
  4. CKD-712

CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway. CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway. CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells. CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer.

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CKD-712

CKD-712 Chemical Structure

CAS No. : 626252-75-3

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CKD-712 Related Antibodies

Top Publications Citing Use of Products

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

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Description

CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway[2]. CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway[1][2]. CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells[1][2]. CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer[1][2][3].

IC50 & Target[1][2]

NF-κB

 

MMP-9

 

IL-6

 

Cdk1/cyclin B

 

CDK1/cyclin A

 

PI3K

 

Akt

 

In Vitro

CKD-712 (5-30 μg/mL; 48 h) dose-dependently suppresses proliferation of A549 human lung adenocarcinoma cells, with 30 μg/mL inhibiting proliferation by 60% without inducing cell death[2].
CKD-712 (30-50 µg/ml; 48 h) induces G2/M cell cycle arrest in A549 cells[2].
CKD-712 (30 µg/ml; 48 h) suppresses cyclin A, cyclin B and CDK-1 expression in A549 human lung cancer cells[2].
CKD-712 (30 µg/ml; 48 h) dose-dependently inhibits mitosis in A549 human lung carcinoma cells[2].
CKD-712 (20 µg/ml; 12 h, 24 h) inhibits adenocarcinoma cell growth[2].
CKD-712 (10 µg/ml; 1 h; pre-incubation) inhibits TNF-α-induced NF-κB activation in A549 human lung carcinoma cells[2].
CKD-712 (5-30 µg/ml; 24 h) suppressed proteins involved in proliferation, anti-apoptosis, and angiogenesis in A549 human lung carcinoma cells[2].
CKD-712 (30 µg/ml; 48 h) dose-dependently inhibits MMP-9 activity in A549 human lung carcinoma cells without affecting MMP-2 activity[2].

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

CKD-712 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: A549 human lung carcinoma cells
Concentration: 5 μg/mL, 10 μg/mL, 20 μg/mL, 30 μg/mL
Incubation Time: 48 h
Result: Significantly suppressed cell proliferation in a dose-dependent manner up to 60% at 30 μg/mL.

Western Blot Analysis[2]

Cell Line: A549 human lung carcinoma cells
Concentration: 5 μg/mL, 10 μg/mL, 20 μg/mL, 30 μg/mL
Incubation Time: 48 h
Result: Suppressed the expression of cyclin A, cyclin B and CDK-1 proteins.

Western Blot Analysis[2]

Cell Line: A549 human lung carcinoma cells
Concentration: 5 μg/mL, 10 μg/mL, 20 μg/mL, 30 μg/mL
Incubation Time: 24 h
Result: Inhibited TNF-α-induced NF-κB p65 nuclear translocation; suppressed proteins involved in proliferation, anti-apoptosis, and angiogenesis including Mcl-1, COX-2, XIAP, and VEGF in A549 cells.

Cell Invasion Assay[2]

Cell Line: A549 human lung carcinoma cells
Concentration: 5 μg/mL, 10 μg/mL, 20 μg/mL, 30 μg/mL
Incubation Time: 24 h
Result: Inhibited A549 cell invasion in a dose-dependent manner.

Cell Migration Assay [2]

Cell Line: A549 human lung carcinoma cells
Concentration: 20 μg/mL
Incubation Time: 12 h, 24 h
Result: Inhibited A549 cell migration as evidenced by controlled wound closure compared to test.

Cell Cycle Analysis[2]

Cell Line: A549 human lung carcinoma cells
Concentration: 5 μg/mL, 10 μg/mL, 20 μg/mL, 30 μg/mL
Incubation Time: 48 h
Result: Induced marked cell cycle changes with an increase in the fraction of cells in G2/M, indicating significant G2/M cell death.
Parmacokinetics
Species Dose Route Note AUClast
Rat[3] 10 mg/kg p.o. 雄性 1172.3 ng·h/mL
Rat[3] 10 mg/kg p.o. 雌性 819.5 ng·h/mL
Rat[3] 3 mg/kg p.o. 雄性 135.2 ng·h/mL
Rat[3] 3 mg/kg p.o. 雌性 135.2 ng·h/mL
Rat[3] 30 mg/kg p.o. 雄性 2721.3 ng·h/mL
Rat[3] 30 mg/kg p.o. 雌性 3520.7 ng·h/mL
In Vivo

CKD-712 (1-20 mg/kg; i.p.; single dose; 30 min pre-LPS) dose-dependently prevents LPS-induced hypothermia in mice, maintaining significantly higher body temperatures at 5 and 7 hours post-LPS challenge[1].
CKD-712 (1-3 mg/kg/day; i.p.; once daily; 4 total doses) improves survival in CLP-induced polymicrobial septic mice, with a 50% survival rate observed at 1 mg/kg/day administered over 4 days[1].
CKD-712 (2.5-20 mg/kg; i.p.; two doses (24 hours and 1 hour pre-LPS)) dose-dependently reduces markers of liver and kidney injury in LPS-induced DIC rats, with the greatest reduction in GOT (117.8 U/L) and BUN (11.8 mg/dL) observed at 20 mg/kg[1].
CKD-712 (20 mg/kg; i.p.; two doses (24 hours and 1 hour pre-LPS)) protects against LPS-induced histological damage to the liver and lung in DIC rats, reducing inflammatory cell infiltration and tissue necrosis[1].
CKD-712 (1-20 mg/kg; i.p.; single dose) dose-dependently improves survival in LPS-induced septic mice, with up to 92% survival observed at 5 and 10 mg/kg when administered 30 minutes pre-LPS[1].
CKD-712 (5-20 mg/kg; i.p.; single dose; 30 min pre-zymosan) improves survival in zymosan-induced septic mice, with a 67% survival rate observed at 20 mg/kg when administered 30 minutes pre-zymosan[1].
CKD-712 (2.5-20 mg/kg; i.p.; two doses (24 hours and 1 hour pre-LPS)) dose-dependently suppresses LPS-induced systemic inflammation in DIC rats, with the greatest reduction in TNF-α (85.5 pg/mL) observed at 10 mg/kg[1].
CKD-712 (20 mg/kg; i.p.; two doses (24 hours and 1 hour pre-LPS)) inhibits LPS-induced NF-κB translocation to the nucleus in lung pneumocytes of DIC rats, reducing pro-inflammatory signaling[1].

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

Animal Model: ICR (male, 25-30 g, zymosan-induced endotoxemia sepsis model)[1]
Dosage: 5, 10, 20 mg/kg
Administration: Intraperitoneal (i.p.) single dose; 30 min pre-zymosan
Result: Achieved survival rates of 42%, 50%, and 67% at 5, 10, and 20 mg/kg respectively at 6 days post-zymosan (statistically significant at 20 mg/kg, p ≤ 0.05).
Animal Model: ICR (male, 25-30 g, LPS-induced hypothermia sepsis model)[1]
Dosage: 1, 3, 10, 20 mg/kg
Administration: Intraperitoneal (i.p.) single dose; 30 min pre-LPS
Result: Prevented LPS-induced hypothermia, maintaining significantly higher mean rectal temperatures compared to vehicle controls at 5 and 7 hours post-LPS (p ≤ 0.05).
Enabled all groups to recover to normal temperatures by 23 hours post-LPS.
Animal Model: ICR (male, 25-30 g, CLP-induced polymicrobial sepsis model)[1]
Dosage: 1, 3 mg/kg/day
Administration: Intraperitoneal (i.p.) once daily; 4 total doses (2 pre-surgery, 2 post-surgery)
Result: Improved final survival rates to 50% and 45% at 1 mg/kg/day and 3 mg/kg/day respectively, compared to 15% survival with CLP alone at 72 hours post-surgery.
Sprague-Dawley (SD) (male, 150–160 g, LPS-induced systemic inflammation Dlc model)
Animal Model: ICR (male, 25-30 g, LPS-induced endotoxemia sepsis model)[1]
Dosage: 1, 3, 10, 20 mg/kg (4 hours post-LPS)
Administration: Intraperitoneal (i.p.) single dose
Result: Achieved survival rates of 33%, 40%, 40%, and 53% at 1, 3, 10, and 20 mg/kg respectively when administered 4 hours post-LPS.
Animal Model: ICR (male, 25-30 g, LPS-induced endotoxemia sepsis model)[1]
Dosage: 2.5, 5, 10, 20 mg/kg (1 hour post-LPS)
Administration: Intraperitoneal (i.p.) single dose
Result: Achieved survival rates of 47%, 60%, 67%, and 67% at 1, 3, 10, and 20 mg/kg respectively when administered 1 hour post-LPS (statistically significant at 10, 20 mg/kg, p ≤ 0.05).
Animal Model: Sprague-Dawley (SD) (male, 150-160 g, LPS-induced septic organ injury Dlc model)[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal (i.p.); two doses (24 hours and 1 hour pre-LPS)
Result: Inhibited LPS-induced translocation of NF-κB from the cytoplasm to the nucleus of lung pneumocytes, with NF-κB remaining localized to the cytoplasm.
Reduced liver sinusoidal enlargement and inflammatory cell infiltration caused by LPS.
Reduced lung pneumocyte hypertrophy, inflammatory cell infiltration, and central necrosis caused by LPS.
Animal Model: Sprague-Dawley (SD) (male, 150–160 g, LPS-induced systemic inflammation Dlc model)[1]
Dosage: 2.5, 5, 10, 20 mg/kg
Administration: Intraperitoneal (i.p.); two doses (24 hours and 1 hour pre-LPS)
Result: LPS-induced GOT, GPT, BUN, creatinine, TNF-α, and IL-6 levels were all reduced in a dose-dependent manner at 2.5, 5, 10, and 20 mg/kg respectively.
Molecular Weight

305.37

Formula

C20H19NO2
CAS No.
SMILES

OC1=CC2=C([C@H](CC3=C(C=CC=C4)C4=CC=C3)NCC2)C=C1O
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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CKD-712 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:

CKD-712626252-75-3CKD712CKD 712Drug DerivativeNF-κBMMPTNF ReceptorInterleukin RelatedCyclin G-associated Kinase (GAK)CDKPI3KAktDrug derivativeNuclear factor-κBNuclear factor-kappaBMatrix metalloproteinasesTumor Necrosis Factor ReceptorTNFRILAuxilin 2Cyclin dependent kinasePhosphoinositide 3-kinasePKBProtein kinase BNF-κB pathway inhibitororally activeA549 cellsSD ratsICR miceLPS-induced sepsis modelcecal ligation and puncture (CLP) modelLPS-induced DIC modeldisseminated intravascular coagulation (DIC)zymosan-induced sepsis model micenon-small cell lung canceranti-inflammatoryanti-sepsisanti-thromboticanti-cancerorgan protectionanti-apoptosiscell cycle arrestselective MMP-9 inhibitionPI3K/Akt signaling activationTNF-α downregulationIL-6 downregulationInhibitorinhibitorinhibit

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