country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-191420

Copy Link Print Information

HDAC3-IN-9

HDAC3-IN-9 is an orally active and selective HDAC3 inhibitor with an IC₅₀ of 22.7 nM. HDAC3-IN-9 selectively targets and inhibits HDAC3 activity, upregulates histone acetylation levels, and blocks the TGF-β/Smad signaling pathway, ultimately inhibiting the expression of pro-fibrotic factors (MMP2, Vimentin, α-SMA, COL1α1, FN1, COL3α1) and attenuating extracellular matrix deposition. HDAC3-IN-9 can be used for research on liver fibrosis.

For research use only. We do not sell to patients.

CAS No.: 3118903-04-8
Formula: C₂₅H₃₃N₃OSi
Molecular Weight:419.63

Storage:

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

Data Sheet (296 KB)

HDAC3-IN-9 Chemical Structure

CAS No.: 3118903-04-8

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

HDAC3

22.7 nM (IC₅₀)

HDAC5

> 10 μM (IC₅₀)

HDAC6

> 10 μM (IC₅₀)

HDAC8

> 10 μM (IC₅₀)

MMP2

Smad3

COL1α1

COL3α1

α-SMA

All HDAC Isoforms :

All TGF-beta/Smad Isoforms :

Smad1
Smad3

All MMP Isoforms :

All Actin Isoforms :

β-Actin

In Vitro

HDAC3-IN-9 (compound 6b) (1 nM-10 μM) is a potent and selective HDAC3 inhibitor in recombinant enzyme assays, with an IC₅₀ of 22.7 nM for HDAC3 and IC₅₀ values of > 10 μM for HDAC5, HDAC6, and HDAC8^[1].
HDAC3-IN-9 (20 μM; 48 h) does not reduce HSC-LX2 viability, with viability retained at > 90%^[1].
HDAC3-IN-9 (2.5-10 μM; 36 h) significantly and dose-dependently inhibits the mRNA expression of pro-fibrotic genes (TIMP3, α-SMA, COL1α1, COL3α1, FN1, COMP) and reduces collagen deposition in TGF-β1 ((HY-P78213))-induced HSC-LX2 cells^[1].
HDAC3-IN-9 (2.5-10 μM; 36 h) dose-dependently reduces the expression levels of fibrosis-related proteins (FN1, MMP2, COL1α1) and cytoskeletal remodeling markers (p-Cofilin, Vimentin, α-SMA) in TGF-β1-induced HSC-LX2 cells^[1].
HDAC3-IN-9 (2.5-10 μM; 36 h) significantly attenuates the expression of profibrotic genes (α-SMA, COL3α1, COL1α1, MMP2, FN1, Vimentin) and proteins in a dose-dependent manner in TGF-β1-induced HHSECs^[1].
HDAC3-IN-9 (10 μM; 36 h) significantly restores histone acetylation levels (H3K27Ac, H4K12Ac, H3K9Ac, H3K14Ac) in TGF-β1-induced HSC-LX2 cells^[1].
HDAC3-IN-9 (2.5-10 μM; 36 h) dose-dependently inhibits p-SMAD3 levels and induces SMAD7 expression in TGF-β1-induced HSC-LX2 cells, thereby suppressing activation of the TGF-β/SMAD signaling pathway^[1].

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

Cell Viability Assay^[1]

Cell Line:

HSC-LX2 cells
Concentration:

20 μM
Incubation Time:

48 h
Result:

Maintained > 90% HSC-LX2 cell viability at 20 μM.

Real Time qPCR^[1]

Cell Line:

HSC-LX2 cells and HHSECs
Concentration:

2.5, 5, 10 μM
Incubation Time:

36 h
Result:

Dose-dependently and significantly downregulated the mRNA expression of key TGF-β-induced profibrotic genes (such as α-SMA, COL1α1, FN1, TIMP3, etc.).

Western Blot Analysis^[1]

Cell Line:

HSC-LX2 cells
Concentration:

2.5, 5, 10 μM
Incubation Time:

36 h
Result:

Dose-dependently decreased the expression of fibrosis and cytoskeletal-related proteins (FN1, MMP2, COL1α1, p-Cofilin, Vimentin) as well as phosphorylated SMAD3 (p-SMAD3), while upregulating SMAD7.
Significantly restored histone acetylation levels (H3K27Ac, H4K12Ac, H3K9Ac, H3K14Ac) at 10 μM.

Immunofluorescence^[1]

Cell Line:

HSC-LX2 cells and HHSECs
Concentration:

2.5, 5, 10 μM
Incubation Time:

36 h
Result:

Dose-dependently and significantly reduced the fluorescence intensity and stress fiber formation of TGF-β-induced α-SMA and Vimentin, indicating reversal of the myofibroblast activation phenotype.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	MRT_{INF_obs}
Mice^[1]	30 mg/kg	p.o.	2.31 h	0.50 h	23.79 ng/mL	67.30 ng·h/mL	3.32 h

In Vivo

HDAC3-IN-9 (compound 6b) (30-60 mg/kg; oral administration; once daily; weeks 5-8) significantly reduces serum liver injury markers, improves the liver morphological index, alleviates histopathological inflammation and collagen deposition, and downregulates the expression of profibrotic and cytoskeletal proteins in the carbon tetrachloride (HY-Y0298)-induced liver fibrosis model in C57BL/6 mice^[1].
HDAC3-IN-9 (2000 mg/kg; oral administration; single dose; 14-day observation) exhibits good safety in normal C57BL/6 mouse models, with no significant body weight changes, no hematological abnormalities, and no gross pathological changes in major organs^[1].

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

Animal Model:

C57BL/6 (male, 6-8 weeks old) received i.p. of 12.5% Carbon tetrachloride (CCl4) in olive oil (at a dose of 2 mL/kg) three times per week for 8 consecutive weeks to induce liver fibrosis^[1]
Dosage:

30 mg/kg; 60 mg/kg
Administration:

p.o.; once daily; weeks 5-8
Result:

Reduced the abnormally elevated serum levels of AST, ALT, and LDH caused by liver injury.
Attenuated the liver and spleen indices (hepatomegaly and splenomegaly) and restored the macroscopic morphological appearance of the liver to near-normal.
Indicated a profound downregulation in the expression levels of profibrotic markers and cytoskeletal remodeling proteins (TGF-β, Desmin, Vimentin, p-Cofilin, COL3α1, α-SMA, TIMP3, FN1, ROCK2) in liver tissues.

Related Protocols :

Chemical Information

CAS No. 3118903-04-8
Molecular Weight 419.63
Formula C₂₅H₃₃N₃OSi
SMILES

CCCCNNC(C1=CC=C(CN2C(CC[Si](C)(C)C3)=C3C4=C2C=CC=C4)C=C1)=O
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (296 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)

References

[1]. Nandawadekar LD, et al. Design, synthesis, and antifibrotic evaluation of silicon-incorporated alkyl hydrazide analogs of tubastatin A: HDAC3 selective inhibitor for ameliorating liver fibrosis. J Med Chem. 2026 Oct 22.

Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote

Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

HDAC3-IN-9

All HDAC Isoforms

All TGF-beta/Smad Isoforms

All MMP Isoforms

All Actin Isoforms