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Art. -Nr.: HY-159172

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HDAC3-IN-4

HDAC3-IN-4 is a selective and orally active HDAC3 inhibitor with an IC₅₀ of 89 nM. HDAC3-IN-4 induces the degradation of PD-L1 by regulating cathepsin B (CTSB) in the lysosomes, with a DC₅₀ of 5.7 μM. HDAC3-IN-4 shows better selectivity for HDAC3 over HDAC1, HDAC6, HDAC7, and HDAC8.

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CAS. Nr.: 2988762-46-3
Formel: C₂₂H₂₅N₅O₂S
Molecular Weight:423.53

Speicherung:

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

Data Sheet (274 KB)

HDAC3-IN-4 Chemical Structure

CAS. Nr.: 2988762-46-3

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

HDAC3

89 nM (IC₅₀)

HDAC1

730 nM (IC₅₀)

HDAC6

>10 μM (IC₅₀)

HDAC7

>10 μM (IC₅₀)

HDAC8

>10 μM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
B16-F10	IC₅₀	1.2 μM Compound: HQ-30	Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay	[PMID: 39031090]
HCT-116	IC₅₀	0.43 μM Compound: HQ-30	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay	[PMID: 39031090]
HepG2	IC₅₀	0.24 μM Compound: HQ-30	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay	[PMID: 39031090]
Jurkat	IC₅₀	0.09 μM Compound: HQ-30	Antiproliferative activity against human Jurkat T cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay Antiproliferative activity against human Jurkat T cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay	[PMID: 39031090]
MCF7	IC₅₀	2.94 μM Compound: HQ-30	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay	[PMID: 39031090]

In Vitro

HDAC3-IN-4 (compound HQ-30) shows potent antiproliferative potency, with IC50 values of 0.09 μM, 0.43 μM, 1.20 μM, 2.94 μM, and 0.24 μM against Jurkat (T lymphoma), HCT-116 (colorectal carcinoma), B16-F10 (melanoma), MCF-7 (breast cancer), and HepG2 (hepatoma) cells, respectively^[1].
HDAC3-IN-4 (0.5-8 μM; 48 h) induces apoptosis in B16-F10 cells in a concentration-dependent manner^[1].
HDAC3-IN-4 (0.5-4 μM; 48 h) dose-dependently increases the percentage of cell cycle arrest in the G2/M phase and reduced the percentage G0/G1 phase in B16-F10 cells^[1].
HDAC3-IN-4 (0.5-4 μM; 24 h) causes significant upregulation of acetylated-H3 (Ac-H3). HDAC3-IN-4 downregulates/degrades PD-L1 expression via the lysosomal pathway^[1].

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

Apoptosis Analysis^[1]

View Protocol

Cell Line:

B16-F10 cells
Concentration:

0.5 μM, 1 μM, 2 μM, 4 μM, and 8 μM
Incubation Time:

48 h
Result:

Induced cancer cell apoptosis.

Cell Cycle Analysis^[1]

View Protocol

Cell Line:

B16-F10 cells
Concentration:

0.5 μM, 1 μM, 2 μM, 4 μM
Incubation Time:

48 h
Result:

Dose-dependently increased the percentage of cell cycle arrest.

Western Blot Analysis^[1]

View Protocol

Cell Line:

B16-F10 cells
Concentration:

0.5 μM, 1 μM, 2 μM, 4 μM
Incubation Time:

24 h
Result:

Caused significant upregulation of acetylated-H3.

In Vivo

HDAC3-IN-4 (compound HQ-30; 25 mg/kg; p.o.; per day; for 9 days) decreases the tumor volume and tumor weight with tumor growth inhibitions^[1].
Pharmacokinetic Parameters of HDAC3-IN-4 in Male Sprague-Dawley rats^[1].
1.19

PK parameters	i.v. administration (2 mg/kg, n = 6)	p.o. administration (20 mg/kg, n = 6)
AUC_0-t (ng/mL·h)	521.85 ± 93.78	2742.08 ± 768.82
AUC_0-∞ (ng/mL·h)	529.16 ± 91.38	3032.62 ± 805.03
MRT_0-t (h)	0.52 ± 0.09	3.19 ± 0.84
MRT_0-∞ (h)	0.55 ± 0.10	4.48 ± 1.75
t_1/2 (h)	0.4 ± 0.10	3.6 ± 1.6
T_max (h)	0.14 ± 0.08	0.50 ± 0
CL (L/h/kg)	3.87 ± 0.65	7.27 ± 3.10
V_z (L/kg)	2.21 ± 0.64	34.45 ± 12.38
C_max (ng/mL)	725.25 ± 169.59	1038.18 ± 514.59
F (%)	-	57

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

Animal Model:

Six weeks old C57BL/6J male mice (6 weeks old) injected B16 cells^[1]
Dosage:

25 mg/kg
Administration:

p.o.; per day; for 9 days
Result:

Decreased the tumor volume and tumor weight with tumor growth inhibitions.

Chemical Information

CAS. Nr. 2988762-46-3
Molecular Weight 423.53
Formel C₂₂H₂₅N₅O₂S
SMILES

O=C(C1=NC=C(CNC2=CC=CC=C2)S1)NCC3=CC=C(C(NNCCC)=O)C=C3
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 (274 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]. Zhiqiang Sun, et al. Discovery of Novel HDAC3 Inhibitors with PD-L1 Downregulating/Degrading and Antitumor Immune Effects. J Med Chem. 2024 Jul 20. [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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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

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HDAC3-IN-4

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Beschreibung

IC50 & Target

Cellular Effect

In Vitro

In Vivo

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

HDAC3-IN-4 Related Classifications

HY-159172 Related Classifications

Bioz

Keywords

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