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Art. -Nr.: HY-183150

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HDAC1-IN-13

HDAC1-IN-13 is an orally active HDAC1 inhibitor with IC₅₀ values of 91, 185, 170, and 280 nM against HDAC1, HDAC2, HDAC3, and HDAC10, respectively, and shows no activity against HDAC4, HDAC5, HDAC6, HDAC7, and HDAC9. HDAC1-IN-13 induces extrinsic apoptosis by activating the caspase-8 pathway and triggers G0/G1 cell cycle arrest. HDAC1-IN-13 can be used for the research of leukemia.

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CAS. Nr.: 3053289-22-5
Formel: C₂₃H₂₀N₄O
Molecular Weight:368.43

Speicherung:

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

HDAC1-IN-13 Chemical Structure

CAS. Nr.: 3053289-22-5

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Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

HDAC1

91 nM (IC₅₀)

HDAC2

181 nM (IC₅₀)

HDAC3

170 nM (IC₅₀)

HDAC10

280 nM (IC₅₀)

Caspase-8

Alle HDAC Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

In Vitro

HDAC1-IN-13 (Compound 6B) potently inhibits HDAC1 (IC₅₀ = 91 nM), HDAC2 (IC₅₀ = 185 nM), HDAC3 (IC₅₀ = 170 nM), and HDAC10 (IC₅₀ = 280 nM) enzymes, with no activity against HDAC4, HDAC5, HDAC7, HDAC8, or HDAC9^[1].
HDAC1-IN-13 (Compound 6B) (72 h) potently inhibits the proliferation of HL-60 (IC₅₀ = 0.31 μM), CCRF-CEM (IC₅₀ = 0.36 μM), and HepG2 (IC₅₀ = 1.01 μM) cancer cells in vitro^[1].
HDAC1-IN-13 (Compound 6B) (72 h) has low cytotoxicity to LO2 normal human hepatocytes (IC₅₀ = 5.67 μM) and a high selectivity index of 18.3 relative to HL-60 cancer cells^[1].
HDAC1-IN-13 (Compound 6B) (0.1-2.5 μM; 48 h) concentration-dependently increases histone H3 acetylation, downregulates Rb/p-Rb and caspase-8 precursor, and modulates BAX, BAK, and BCL-2 expression in HL-60 cells after 48 h of treatment^[1].
HDAC1-IN-13 (Compound 6B) (0-2.5 μM; 48 h) concentration-dependently induces apoptosis in HL-60 cells, with a 46.1% apoptosis rate following 48 h treatment with 2.5 μM^[1].
HDAC1-IN-13 (Compound 6B) (0-2.5 μM; 48 h) concentration-dependently induces G₀/G₁ phase cell cycle arrest in HL-60 cells, with 76.5% of cells arrested in G₀/G₁ following 48 h treatment with 2.5 μM^[1].

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

Western Blot Analysis^[1]

Cell Line:

HL-60 promyelocytic leukemia cells
Concentration:

0.1 μM, 0.5 μM, 2.5 μM
Incubation Time:

48 h
Result:

Induced a concentration-dependent increase in acetylated histone H3 (Ac-H3) levels, while total histone H3 levels remained unchanged.
Downregulated expression of Rb, phosphorylated Rb (p-Rb), and caspase-8 precursor in a concentration-dependent manner.
Downregulated BAX, BAK, and BCL-2 expression.

Apoptosis Analysis^[1]

Cell Line:

HL-60 promyelocytic leukemia cells
Concentration:

0 μM, 0.1 μM, 0.5 μM, 2.5 μM
Incubation Time:

48 h
Result:

Induced apoptosis in a concentration-dependent manner, with apoptosis rates of 13.87% (0 μM), 25.6% (0.1 μM), 27.6% (0.5 μM), and 46.1% (2.5 μM).
Reached a late apoptotic cell proportion of 22.7% at the highest concentration.

Cell Cycle Analysis^[1]

Cell Line:

HL-60 promyelocytic leukemia cells
Concentration:

0 μM, 0.1 μM, 0.5 μM, 2.5 μM
Incubation Time:

48 h
Result:

Induced G₀/G₁ phase cell cycle arrest in a concentration-dependent manner, with the proportion of cells in G₀/G₁ phase increasing from 56.4% (0 μM) to 76.5% (2.5 μM).

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC	AUC_0-∞	MRT	V_d	CL
Rat^[1]	14 mg/kg	i.p.	10.88 h	0.67 h	3085.04 μg/L	9195.38 μg/L·h	9455.28 μg/L·h	6.67 h	23.25 L/kg	1.48 L/h/kg
Rat^[1]	14 mg/kg	i.g.	5.01 h	1.50 h	511.88 μg/L	4332.53 μg/L·h	4350.86 μg/L·h	6.05 h	23.25 L/kg	3.22 L/h/kg

In Vivo

HDAC1-IN-13 (Compound 6B) (15-30 mg/kg; p.o.; once daily; 18 days) exhibits significant in vivo anti-leukemic activity in mouse models after oral administration, with no obvious toxicity^[1].
HDAC1-IN-13 (20 mg/kg; i.p.; once daily; for 7 consecutive days) exhibits potent in vivo anti-leukemia activity with no obvious toxicity in mouse models following intraperitoneal administration^[1].

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

Animal Model:

BALB/c nude (male, 6-8 weeks old, 18-22 g, subcutaneous xenograft model)^[1]
Dosage:

15 mg/kg; 30 mg/kg
Administration:

i.g.; daily; 18 days
Result:

Achieved a tumor growth inhibition (TGI) rate of 20.72% at 30 mg/kg.
Showed no obvious pathological changes in heart, liver, spleen, lung, or kidney tissue.
Maintained stable mouse body weights throughout the study.

Animal Model:

BALB/c nude (male, 6-8 weeks old, 18-22 g, subcutaneous xenograft model)^[1]
Dosage:

20 mg/kg
Administration:

i.p.; daily; 7 days
Result:

Reduced tumor volume by 58.4% after 7 days.
Showed no changes in mouse body weight during the study, indicating low in vivo toxicity.

Chemical Information

CAS. Nr. 3053289-22-5
Molecular Weight 368.43
Formel C₂₃H₂₀N₄O
SMILES

O=C(NC1=CC=CC=C1N)C(C=C2)=CC=C2CNC3=CC=NC4=CC=CC=C43
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]. Yu B, et al. Synthesis and evaluation of novel N-arylamide-quinoline derivatives as HDAC isoform-selective inhibitors: in vitro and in vivo anticancer efficacy and pharmacokinetic studies. Bioorg Chem. 2026;176:109877. [Content Brief]

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.

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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HDAC1-IN-13

Alle HDAC Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

HDAC1-IN-13 Related Classifications

HY-183150 Related Classifications