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Art. -Nr.: HY-189233

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KZL-064

KZL-064 is an orally active HDAC1 ligand that directly binds to HDAC1. KZL-064 inhibits the proliferation, migration, and invasion of hepatocellular carcinoma cells, and induces apoptosis and G2/M phase cell cycle arrest. The antiproliferative, proapoptotic, and cell cycle regulatory effects of KZL-064 are partially dependent on HDAC1, while its inhibitory effects on migration and invasion also involve HDAC1-independent mechanisms. KZL-064 is applicable to hepatocellular carcinoma research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2773345-67-6
Formel: C₁₇H₁₅F₃N₄O
Molecular Weight:348.32

Speicherung:

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

KZL-064 Chemical Structure

CAS. Nr.: 2773345-67-6

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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]

HDAC1

7.54 × 10< (Kd)

Alle HDAC Isoform-spezifische Produkte anzeigen :

In Vitro

KZL-064 (2.5 or 10 nM; up to 4 days) inhibits the proliferation/viability of MHCC97-H and HUH7 cells in a time- and dose-dependent manner^[1].
KZL-064 (2.0 nM; 24 h) inhibits colony formation in MHCC97-H and HUH7 cells, but does not affect the clonal growth of normal LX2 cells^[1].
KZL-064 (1-2.5 nM; 24 h) exerts a significant anti-migratory effect on MHCC97-H and HUH7 hepatocellular carcinoma cells at nanomolar concentrations^[1].
KZL-064 (1-2.5 nM; 24 h) significantly impairs the invasive capacity of MHCC97-H human hepatocellular carcinoma cells at low nanomolar concentrations^[1].
Under the same exposure conditions, KZL-064 exerts a stronger antiproliferative effect on HDAC1-overexpressing MHCC97-H cells, while HDAC1 knockdown only slightly reduces cellular sensitivity to KZL-064; HDAC1 knockdown does not abrogate the inhibitory effect of KZL-064 on cell migration and invasion^[1].
KZL-064 (1-10 nM; 1 h) directly and preferentially binds to the HDAC1 protein in MHCC97-H cells to enhance its thermal stability, and no interaction with HDAC2 or HDAC8 is detected under the same experimental conditions^[1].
KZL-064 (10-50 μM) binds to recombinant HDAC1 protein in a concentration-dependent manner in BLI assays, with a K_D of 7.54 × 10^-5^[1].
KZL-064 (2.5-10 nM; 24 h) induces G₂/M phase arrest in MHCC97-H cells, a process that is partially dependent on HDAC1; even when HDAC1 expression is knocked down, this compound still retains significant anti-proliferative and pro-apoptotic activities^[1].
KZL-064 (2.5 nM; 24 h) induces significant G2/M phase arrest in MHCC97-H cells, while HDAC1 knockdown partially reverses this cell cycle arrest^[1].

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

Cell Viability Assay^[1]

Cell Line:

MHCC97-H; HUH7
Concentration:

2.5, 10 nM
Incubation Time:

Up to 4 days
Result:

Reduced cell viability in a time- and dose-dependent manner in both cell lines.

Cell Proliferation Assay^[1]

Cell Line:

MHCC97-H; HUH7; LX2
Concentration:

2 nM
Incubation Time:

24 h
Result:

Suppressed colony formation in MHCC97-H and HUH7 cells.
Did not affect clonogenic growth of normal LX2 cells.

Cell Migration Assay ^[1]

Cell Line:

MHCC97-H; HUH7
Concentration:

1 nM, 2.5 nM
Incubation Time:

24 h
Result:

Reduced migration of MHCC97-H cells.
Reduced migration of HUH7 cells.

Cell Invasion Assay^[1]

Cell Line:

MHCC97-H
Concentration:

1 nM, 2.5 nM
Incubation Time:

24 h
Result:

Reduced invasion of MHCC97-H cells.

Cell Cycle Analysis^[1]

Cell Line:

MHCC97-H
Concentration:

2.5 nM
Incubation Time:

24 h
Result:

Induced pronounced G2/M-phase arrest.
HDAC1 knockdown partially attenuated the G2/M-phase arrest.

Apoptosis Analysis^[1]

Cell Line:

MHCC97-H
Concentration:

2.5, 10 nM
Incubation Time:

24 h
Result:

Increased apoptosis.
Produced greater apoptosis in HDAC1-overexpressing cells.
HDAC1 knockdown partially attenuated the apoptotic response.

Western Blot Analysis^[1]

Cell Line:

MHCC97-H
Concentration:

1-10 nM
Incubation Time:

1 h
Result:

Increased HDAC1 thermal stability in CETSA.
Did not produce appreciable thermal stabilization of HDAC2 or HDAC8 under the tested temperature conditions.

In Vivo

KZL-064 (0.5-2.0 μg/kg; intragastric administration; once every 2 days; for 14 consecutive days) exerts a dose-dependent inhibitory effect on tumor growth and reduces tumor volume and weight in a subcutaneous MHCC97-H xenograft model in 4-week-old male BALB/c nude mice. The tumor inhibitory effect in the 2.0 μg/kg group is comparable to that of the 20 mg/kg positive control group, while no significant effect on body weight or major organ weights is observed. KZL-064 decreases cell density and increases necrotic areas in MHCC97-H xenograft tumor tissues, downregulates Ki-67 expression, upregulates p53 expression, and does not alter HDAC1 expression^[1].

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

Animal Model:

BALB/c nude mice (4-week-old male)^[1]
Dosage:

0.5 μg/kg; 1.0 μg/kg; 2.0 μg/kg
Administration:

i.g.; every 2 days; 14 days
Result:

Exhibited dose-dependent tumor growth inhibition.
Showed anti-tumor efficacy comparable to sorafenib at microgram-per-kilogram doses.
Caused no reduction in mouse body weight at the highest tested dose.
Produced no significant differences in organ weight or organ histology compared to vehicle control groups.
Induced reduced tumor cellularity and increased necrotic areas in H&E stained tumor sections.
Did not alter HDAC1 expression levels, significantly reduced Ki-67 expression, and significantly elevated p53 expression in subcutaneous tumor sections.

Chemical Information

CAS. Nr. 2773345-67-6
Molecular Weight 348.32
Formel C₁₇H₁₅F₃N₄O
SMILES

COC1=CC=C(C=C1N)N(C2=NC(C(F)(F)F)=NC3=CC=CC=C32)C
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

Handling Instructions (2659 KB)

Verweise

[1]. Wang S, et al. A trifluoromethyl quinazoline inhibits hepatocellular carcinoma proliferation through HDAC1 binding and multi-target mechanisms. iScience. 2026 Aug 21;29(8):117037.

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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