Home Epigenetics HDAC inhibitor Tucidinostat (Chidamide) For research use only.

Tucidinostat (Chidamide)

Synonyms: HBI-8000, CS-055

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.

Tucidinostat (Chidamide) Chemical Structure

Tucidinostat (Chidamide) Chemical Structure

CAS No. 1616493-44-7

Purity & Quality Control

Tucidinostat (Chidamide) Related Products

Signaling Pathway

HDAC Signaling Pathways

HDAC Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 Function assay 5 mins Inhibition of recombinant human full length HDAC1 expressed in baculovirus infected Sf9 insect cells using biotinylated lysine 9 acetylated histone H3 (1 to 21 residues) as substrate incubated for 5 mins followed by substrate addition measured after 60 mi, IC50 = 0.112 μM. 28835797
EBC1 Antiproliferative assay 72 hrs Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay, IC50 = 2.9 μM. 28835797
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50 = 7.8 μM. 28835797
HL60 Growth inhibition assay 48 hrs Growth inhibition of human HL60 cells incubated for 48 hrs by MTS method, GI50 = 0.4 μM. ChEMBL
Jurkat Growth inhibition assay 48 hrs Growth inhibition of human Jurkat cells incubated for 48 hrs by MTS method, GI50 = 1.5 μM. ChEMBL
hematopoietic malignant cells Cytotoxicity assay Cytotoxicity against human hematopoietic malignant cells assessed as growth inhibition, GI50 = 1.86 μM. ChEMBL
U2OS Growth inhibition assay 48 hrs Growth inhibition of human U2OS cells incubated for 48 hrs by MTS method, GI50 = 2 μM. ChEMBL
HepG2 Growth inhibition assay 48 hrs Growth inhibition of human HepG2 cells incubated for 48 hrs by MTS method, GI50 = 4 μM. ChEMBL
LNCAP Growth inhibition assay 48 hrs Growth inhibition of human LNCAP cells incubated for 48 hrs by MTS method, GI50 = 4 μM. ChEMBL
Raji Growth inhibition assay 48 hrs Growth inhibition of human Raji cells incubated for 48 hrs by MTS method, GI50 = 4 μM. ChEMBL
MCF7 Growth inhibition assay 48 hrs Growth inhibition of human MCF7 cells incubated for 48 hrs by MTS method, GI50 = 5 μM. ChEMBL
28SC Growth inhibition assay 48 hrs Growth inhibition of human 28SC cells incubated for 48 hrs by MTS method, GI50 = 5.8 μM. ChEMBL
PANC1 Growth inhibition assay 48 hrs Growth inhibition of human PANC1 cells incubated for 48 hrs by MTS method, GI50 = 6.3 μM. ChEMBL
human solid tumor cells Cytotoxicity assay Cytotoxicity against human solid tumor cells assessed as growth inhibition, GI50 = 6.65 μM. ChEMBL
HeLa Function assay 10 mins Inhibition of HDAC enzymatic activity in human HeLa cells incubated for 10 mins in presence of substrate by colorimetric activity assay, IC50 = 7.2 μM. ChEMBL
MDA-MB-231 Growth inhibition assay 48 hrs Growth inhibition of human MDA-MB-231 cells incubated for 48 hrs by MTS method, GI50 = 7.9 μM. ChEMBL
SMMC7721 Growth inhibition assay 48 hrs Growth inhibition of human SMMC7721 cells incubated for 48 hrs by MTS method, GI50 = 16 μM. ChEMBL
DU145 Growth inhibition assay 48 hrs Growth inhibition of human DU145 cells incubated for 48 hrs by MTS method, GI50 = 25 μM. ChEMBL
HeLa Growth inhibition assay 48 hrs Growth inhibition of human HeLa cells incubated for 48 hrs by MTS method, GI50 = 40 μM. ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of PPARG (unknown origin) expressed in human U2OS cells at 1 uM in presence of 10 uM rosiglitazone incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of ERbeta (unknown origin) expressed in human U2OS cells at 1 uM in presence of 0.01 uM E2 incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of glulcocorticoid receptor (unknown origin) expressed in human U2OS cells at 1 uM in presence of 0.1 uM dexamethasone incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of ERalpha (unknown origin) expressed in human U2OS cells at 1 uM in presence of 0.01 uM E2 incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of glulcocorticoid receptor (unknown origin) expressed in human U2OS cells at 1 uM incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of PPARG (unknown origin) expressed in human U2OS cells at 1 uM incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of ERalpha (unknown origin) expressed in human U2OS cells at 1 uM incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of ERbeta (unknown origin) expressed in human U2OS cells at 1 uM incubated for 24 hrs by luciferase reporter gene assay ChEMBL
Click to View More Cell Line Experimental Data

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.
Targets
HDAC3 [1]
(Cell-free)		 HDAC10 [1]
(Cell-free)		 HDAC1 [1]
(Cell-free)		 HDAC2 [1]
(Cell-free)
67 nM 78 nM 95 nM 160 nM
In vitro
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].
Cell Research 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).
Experimental Result Images Methods Biomarkers Images PMID
Western blot PARP / Cleaved PARP / Caspase-3 / Cleaved caspase-3 p-EGFR / EGFR / p-STAT3 / STAT3 / p-AKT / AKT / p-AMPK / MAPK Ace-H3K18 / Ace-H3K9 / Ac-H4K8 Mcl-1 / Myc / Bcl-xl / p21 / p27 / CDK6 / CDK4 / Cyclin D2 HDAC1 / HDAC2 / HDAC3 / acetyl-H3 / acetyl-H4 30854137
Growth inhibition assay Cell viability 29100410
In Vivo
In vivo

In HCT-8 colorectal carcinoma mice xenografts, Chidamide shows in vivo antitumor activity. However, chidamide is well-tolerated at the above doses in the tumor-bearing animals, whereas the control drugs cause significant weight loss[1].
Animal Research Animal Models Athymic nude mice (BALB/c-nu)
Dosages 12.5-50 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05586841 Not yet recruiting
HR+/HER2- Advanced Breast Cancer
Beijing 302 Hospital
 November 1 2022 Phase 1
NCT05141357 Terminated
Non Small Cell Lung Cancer
HUYABIO International LLC.
 March 14 2022 Phase 2
NCT04994210 Recruiting
Safety and Efficacy
Sun Yat-sen University
 October 4 2021 Phase 2
NCT05140616 Recruiting
Safety and Efficacy
The First Affiliated Hospital of Soochow University
 May 31 2021 Phase 1|Phase 2
NCT04651127 Unknown status
Cervical Cancer|Cervix Cancer|Cervix Neoplasm
Sun Yat-sen University
 November 9 2020 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 390.41 Formula

C22H19FN4O2
CAS No. 1616493-44-7 SDF Download Tucidinostat (Chidamide) SDF
Smiles C1=CC(=CN=C1)C=CC(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 78 mg/mL ( (199.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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