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Art. -Nr.: HY-188346

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₃₄H₃₇ClN₄O₂
Molecular Weight:569.14

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (298 KB)

KZ-5 Chemical Structure

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

DNMT1

Alle DNA Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

KZ-5 (1-5 μM; 48 h) inhibits fibrosis-related markers, with weak inhibitory effect on HSC activation^[1].
KZ-5 binds to PROTAC as a ligand and competitively blocks the binding of PROTAC to DNMT1, rescuing PROTAC-mediated degradation^[1].

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

RT-PCR^[1]

Cell Line:

human LX-2 hepatic stellate cells
Concentration:

1 and 5 μM
Incubation Time:

48 h
Result:

Only weakly suppressed HSC activation.

In Vivo

KZ-5 (30 mg/kg; i.p.; once every two days; 3 weeks) in the CCl4 (HY-Y0298)-induced liver fibrosis model reduces α-SMA and Collagen I, but does not degrade DNMT1 and does not restore fibrosis and injury indicators to normal^[1].
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.

Animal Model:

C57BL/6J (male, 6-8 weeks)^[1]
Dosage:

30 mg/kg
Administration:

i.p.; once every two days; 3 weeks
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.

Animal Model:

C57BL/6N (male, 6-8 weeks)^[1]
Dosage:

30 mg/kg
Administration:

i.p.; every other day; 7 days after BDL
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.

Related Protocols :

Chemical Information

Molecular Weight 569.14
Formel C₃₄H₃₇ClN₄O₂
SMILES

OC(CN1CCNCC1)COC(CN2C3=C(C4=C2C=CC=C4)C=CC=C3)CN5C6=C(C7=CC=CC=C75)C=CC=C6.Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (298 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Su X, et al. Discovery of Potent, Selective DNMT1 PROTAC Degraders: Simultaneous Blockade of Catalytic and Non-Catalytic Functions for Liver Fibrosis Therapy. Journal of medicinal chemistry. 2026 Oct 22;69(20):23387-23410.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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