Tucidinostat (Chidamide)

For research use only.

Catalog No.S8567 Synonyms: HBI-8000, CS-055

2 publications

Tucidinostat (Chidamide) Chemical Structure

CAS No. 1616493-44-7

Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.

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Selleck's Tucidinostat (Chidamide) has been cited by 2 publications

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Biological Activity

Description Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.
HDAC3 [1]
HDAC10 [1]
HDAC1 [1]
HDAC2 [1]
67 nM 78 nM 95 nM 160 nM
In vitro

Chidamide inhibits class I HDACs 1-3, as well as class IIb HDAC10, at low nanomolar concentrations. Chidamide significantly induces histone H3 acetylation in both HeLa human cervical adenocarcinoma cells and human PBMC. Cell growth inhibition studies performed with 18 human-derived tumor cell lines demonstrate that chidamide and MS-275 similarly inhibit the in vitro growth of most, but not all, tumor cells in the low micromolar concentration range. However, chidamide, and to a lesser extent MS-275, is significantly less toxic to normal cells from human fetal kidney (CCC-HEK) and liver (CCC-HEL), indicating a differential cytotoxic response of normal cells versus cancerous cells to chidamide[1].

Methods Test Index PMID
Western blot
PARP / Cleaved PARP / Caspase-3 / Cleaved caspase-3 ; 

PubMed: 30854137     

Expression and activation level of Caspase-3 and PARP after treatment of serial dilutions of chidamide in HCC827 cells (48h).

p-EGFR / EGFR / p-STAT3 / STAT3 / p-AKT / AKT / p-AMPK / MAPK ; 

PubMed: 30854137     

Chidamide inhibition of PTK signaling molecules in A549 cells (48h).

Ace-H3K18 / Ace-H3K9 / Ac-H4K8 ; 

PubMed: 29773595     

Western blot analysis of H3 acetylation at Lys18 and Lys9 and H4 acetylation at Lys8. H3 and H4 expression levels were used as loading controls. 

Mcl-1 / Myc / Bcl-xl / p21 / p27 / CDK6 / CDK4 / Cyclin D2 ; 

PubMed: 29773595     

Western blot analysis of Mcl-1, Myc, Bcl-xL, Bcl-2, p21, p27, CDK4, CDK6, and Cyclin-D2 levels; α-tubulin was used as the loading control. 

HDAC1 / HDAC2 / HDAC3 / acetyl-H3 / acetyl-H4 ; 

PubMed: 31289512     

(A) RPMI8226 cells were treated with 0, 0.5, 1 or 2 µmol/l chidamide for 48 h and (B) U266 cells were treated with 0, 2, 4 or 8 µmol/l chidamide for 48 h, and HDACs expression was assessed using western blot analysis.

30854137 29773595 31289512
Growth inhibition assay
Cell viability; 

PubMed: 29100410     

(a) Proliferation rates at 24, 48, 72 hour of Hs445 cells after treated with 0.1μM, 0.3μM, 1μM, 3μM, 10μM, 30μM Chidamides; (b) proliferation rates at 24, 48, 72 hours of L428 cells after treated with 0.1μM, 0.3μM, 1μM, 3μM, 10μM, 30μM Chidamide;

In vivo In HCT-8 colorectal carcinoma mice xenografts, Chidamide shows in vivo antitumor activity. Chidamide in the dose range of 12.5-50 mg/kg dose-dependently reduces tumor size and tumor weight, and the dose of 50 mg/kg produces similar or greater efficacy compared with the control drugs 5-fluorouracil(5-FU, 20 mg/kg) and MS-275 (25 mg/kg, which was reported as the maximum tolerated dose in xenograft models). However, chidamide is well-tolerated at the above doses in the tumor-bearing animals, whereas the control drugs cause significant weight loss[1].


Cell Research:


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  • Cell lines: PBMC effector cells
  • Concentrations: 0-400 nM
  • Incubation Time: 0-400 nM
  • Method:

    Isolated PBMC effector cells are seeded into 6-well plates (6 x 106 cells/well) and treated with chidamide at different concentrations (0-400 nM) for different times (24-72 h).

    (Only for Reference)
Animal Research:


- Collapse
  • Animal Models: Athymic nude mice (BALB/c-nu)
  • Dosages: 12.5-50 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (199.78 mM)
Water Insoluble
Ethanol '2 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC Na
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 390.41


CAS No. 1616493-44-7
Storage powder
in solvent
Synonyms HBI-8000, CS-055
Smiles C1=CC(=CN=C1)C=CC(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03820596 Recruiting Drug: Sintilimab|Drug: Chidamide Safety and Efficacy Huiqiang Huang|Sun Yat-sen University March 29 2019 Phase 1|Phase 2
NCT02944812 Unknown status Drug: Chidamide Peripheral T Cell Lymphoma Guangdong Provincial People''s Hospital March 2016 Phase 2
NCT02569489 Withdrawn Drug: HBI-8000|Drug: Trastuzumab|Drug: Paclitaxel Breast Cancer HUYA Bioscience International December 2015 Phase 1
NCT02513901 Completed Drug: Chidamide Chronic HIV Infections Tang-Du Hospital|Chipscreen Biosciences Ltd. August 2015 Phase 1|Phase 2
NCT02482753 Active not recruiting Drug: Chidamide|Drug: exemestane|Drug: placebo Breast Cancer Chipscreen Biosciences Ltd. July 2015 Phase 3

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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID