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 Chemical Structure

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)

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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