2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. 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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HDAC3-IN-4

HDAC3-IN-4 Chemical Structure

CAS No. : 2988762-46-3

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HDAC3-IN-4 Related Antibodies

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Description

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[1].

IC50 & Target[1]

HDAC3

89 nM (IC50)

HDAC1

730 nM (IC50)

HDAC6

>10 μM (IC50)

HDAC7

>10 μM (IC50)

HDAC8

>10 μM (IC50)

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.

HDAC3-IN-4 Related Antibodies

Apoptosis Analysis[1]

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]

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]

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)
AUC0-t (ng/mL·h) 521.85 ± 93.78 2742.08 ± 768.82
AUC0-∞ (ng/mL·h) 529.16 ± 91.38 3032.62 ± 805.03
MRT0-t (h) 0.52 ± 0.09 3.19 ± 0.84
MRT0-∞ (h) 0.55 ± 0.10 4.48 ± 1.75
t1/2 (h) 0.4 ± 0.10 3.6 ± 1.6
Tmax (h) 0.14 ± 0.08 0.50 ± 0
CL (L/h/kg) 3.87 ± 0.65 7.27 ± 3.10
Vz (L/kg) 2.21 ± 0.64 34.45 ± 12.38
Cmax (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.
Molecular Weight

423.53

Formula

C22H25N5O2S
CAS No.
SMILES

O=C(C1=NC=C(CNC2=CC=CC=C2)S1)NCC3=CC=C(C(NNCCC)=O)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HDAC3-IN-4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HDAC3-IN-42988762-46-3HDACHistone deacetylasesHDAC3 InhibitorAntitumor Immune EffectsPD-L1Inhibitorinhibitorinhibit

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