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HDAC3-IN-4

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Catalog No. T89627Cas No. 2988762-46-3

HDAC3-IN-4 is a selective and orally active inhibitor of HDAC3, boasting an IC50 of 89 nM. It induces the degradation of PD-L1 by modulating cathepsin B (CTSB) in lysosomes, with a DC50 of 5.7 μM. Compared to HDAC1, HDAC6, HDAC7, and HDAC8, HDAC3-IN-4 demonstrates superior selectivity for HDAC3.

HDAC3-IN-4

HDAC3-IN-4

😃Good
Catalog No. T89627Cas No. 2988762-46-3
HDAC3-IN-4 is a selective and orally active inhibitor of HDAC3, boasting an IC50 of 89 nM. It induces the degradation of PD-L1 by modulating cathepsin B (CTSB) in lysosomes, with a DC50 of 5.7 μM. Compared to HDAC1, HDAC6, HDAC7, and HDAC8, HDAC3-IN-4 demonstrates superior selectivity for HDAC3.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mgInquiry10-14 weeks10-14 weeks
50 mgInquiry10-14 weeks10-14 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
HDAC3-IN-4 is a selective and orally active inhibitor of HDAC3, boasting an IC50 of 89 nM. It induces the degradation of PD-L1 by modulating cathepsin B (CTSB) in lysosomes, with a DC50 of 5.7 μM. Compared to HDAC1, HDAC6, HDAC7, and HDAC8, HDAC3-IN-4 demonstrates superior selectivity for HDAC3.
Targets&IC50
HDAC1:730 nM, HDAC6:>10 μM, HDAC8:>10 μM, HDAC7:>10 μM, HDAC3:89 nM
In vitro
HDAC3-IN-4 (compound HQ-30) exhibits potent antiproliferative effects, with IC50 values of 0.09 μM for Jurkat (T lymphoma), 0.43 μM for HCT-116 (colorectal cancer), 1.20 μM for B16-F10 (melanoma), 2.94 μM for MCF-7 (breast cancer), and 0.24 μM for HepG2 (liver cancer). At concentrations ranging from 0.5 to 8 μM over 48 hours, HDAC3-IN-4 induces apoptosis in B16-F10 cells in a concentration-dependent manner. Furthermore, at doses from 0.5 to 4 μM for 48 hours, it increases the percentage of B16-F10 cells in the G2/M phase of the cell cycle, while decreasing the percentage in the G0/G1 phase. Additionally, at 0.5 to 4 μM for 24 hours, HDAC3-IN-4 significantly upregulates acetylated H3 (Ac-H3). The compound also modulates PD-L1 expression through the lysosomal pathway.
In vivo
HDAC3-IN-4 (compound HQ-30; 25 mg/kg; oral administration; daily; for 9 days) effectively decreases tumor volume and weight, consequently inhibiting tumor growth.
Chemical Properties
Molecular Weight423.53
FormulaC22H25N5O2S
Cas No.2988762-46-3
SmilesO=C(NCC1=CC=C(C=C1)C(=O)NNCCC)C2=NC=C(S2)CNC=3C=CC=CC3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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