KZ-5
KZ-5 is a DNMT1 binder that competitively blocks the binding of PROTAC to DNMT1, rescuing PROTAC-mediated degradation. KZ-5 weakly inhibits hepatic stellate cell activation. KZ-5 partially reduces classical tissue fibrosis markers in liver fibrosis models. KZ-5 can be used in research related to liver fibrosis.
For research use only. We do not sell to patients.
- Formula: C34H37ClN4O2
- Molecular Weight:569.14
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All DNA Methyltransferase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
DNMT1 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human LX-2 hepatic stellate cells
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Concentration:1 and 5 μM
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Incubation Time:48 h
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Result:Only weakly suppressed HSC activation.
In Vivo
KZ-5 (30 mg/kg; i.p.; once every other day; 7 days) does not degrade DNMT1, does not reduce α-SMA, and does not restore fibrosis, injury markers, survival, or body weight to normal in BDL-induced cholestatic liver fibrosis in C57BL/6N mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 6-8 weeks)[1]
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Dosage:30 mg/kg
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Administration:i.p.; once every two days; 3 weeks
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Result:Did not reduce hepatic DNMT1 protein below CCl4-induced levels.
Lowered hepatic α-SMA and Collagen I protein versus CCl4, but Sirius Red collagen staining remained elevated and was not reduced versus CCl4.
Serum ALT, AST, and ALB were not normalized to oil-control levels; body weight remained below the oil group, and the liver-to-body weight ratio remained above oil-control levels.
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Animal Model:C57BL/6N (male, 6-8 weeks)[1]
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Dosage:30 mg/kg
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Administration:i.p.; every other day; 7 days after BDL
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Result:Did not reduce hepatic DNMT1 protein versus BDL.
Hepatic α-SMA remained elevated and was not reduced versus BDL.
Did not reduce Sirius Red collagen staining versus BDL, and serum ALT, AST, and bilirubin remained elevated rather than returning to Sham levels.
Survival and body weight were not normalized to Sham levels.
Chemical Information
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Molecular Weight 569.14
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Formula C34H37ClN4O2
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SMILES
OC(CN1CCNCC1)COC(CN2C3=C(C4=C2C=CC=C4)C=CC=C3)CN5C6=C(C7=CC=CC=C75)C=CC=C6.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KZ-5 Related Classifications
HY-188346 Related Classifications
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