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Tucidinostat (Chidamide) HDAC inhibitor

Cat.No.S8567

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. It exhibits IC50 values of 95, 160, 67, and 78 nM for HDAC1, 2, 3, and 10, respectively.
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Quality Control

Batch: Purity: 99.99%
99.99

Cell Culture, Treatment & Working Concentration

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
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Solubility

In vitro
Batch:

DMSO : 78 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 390.41 Formula

C22H19FN4O2

Storage (From the date of receipt)
CAS No. 1616493-44-7 Download SDF Storage of Stock Solutions

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

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
HDAC3
(Cell-free)
67 nM
HDAC10
(Cell-free)
78 nM
HDAC1
(Cell-free)
95 nM
HDAC2
(Cell-free)
160 nM
In vitro

Tucidinostat (Chidamide) inhibits class I HDACs 1-3, as well as class IIb HDAC10, at low nanomolar concentrations. It 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 this compound and MS-275 similarly inhibit the in vitro growth of most, but not all, tumor cells in the low micromolar concentration range. However, it, 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.

In vivo

In HCT-8 colorectal carcinoma mice xenografts, Tucidinostat (Chidamide) shows in vivo antitumor activity. However, it is well-tolerated at the above doses in the tumor-bearing animals, whereas the control drugs cause significant weight loss.

References

Applications

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
S8567-WB1
30854137
Growth inhibition assay Cell viability
S8567-viability1
29100410

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-09-15)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06947967 RECRUITING
Lymphoma, T-Cell, Peripheral
Chipscreen Biosciences, Ltd.
2025-08-12 PHASE3
NCT05088226 RECRUITING
Peripheral Blood Stem Cell Transplantation
Chinese PLA General Hospital
2021-12-01 PHASE2
NCT07598578 RECRUITING
Peripheral T-Cell Lymphoma Refractory
Second Affiliated Hospital of Soochow University
2026-06-01 EARLY_PHASE1
NCT06890585 NOT_YET_RECRUITING
BTK Inhibitors; Histone Deacetylase Inhibitor; Double Express Diffuse Large B-cell Lymphoma
Li Zhiming
2025-06-01 PHASE2
NCT06674096 RECRUITING
Double-expressor Lymphoma
Zhejiang Cancer Hospital
2024-11-06 PHASE2
NCT07493148 RECRUITING
Diffuse Large B-Cell Lymphoma (DLBCL)
Ou Bai, MD/PHD
2026-04-30 PHASE2

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