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Datasheet of Chidamide
Description:.
Chidamide(CS055; HBI-8000) is a class I HDAC inhibitor with IC50s of 95/160/67/733 nM for HDAC1/2/3/8; also inhibits
HDAC10/11(IC50=78/432 nM); no inhibition on HDAC4/5/7/9/6(IC50>30 uM).
in vitro: Chidamide was able to increase the acetylation levels of histone H3 and to inhibit the PI3K/Akt and MAPK/Ras
signaling pathways, which resulted in arresting colon cancer cells at the G1 phase of the cell cycle and promoting apoptosis.
chidamide inhibited class I HDACs 13, as well as class IIb HDAC10, at low nanomolar concentrations. Chidamide significantly
induced histone H3 acetylation in both HeLa human cervical adenocarcinoma cells and human PBMC and the extent of induction
was similar to that seen with MS-275 and SAHA. Cell growth inhibition studies performed with 18 human-derived tumor cell
lines demonstrated that chidamide and MS-275 similarly inhibited the in vitro growth of most, but not all, tumor cells in the low
micromolar concentration range. At low concentrations (<1 M), CS055 induced G1 arrest. At moderate concentrations (0.5
M-2 M), CS055 induced differentiation, as determined by the increased expression of the myeloid differentiation marker
CD11b. At relatively high concentrations (2 M-4 M), CS055 potently induced caspase-dependent apoptosis. Chidamide
treatment significantly decreased the expression of type I HDACs, uncleaved Caspase-3 and p21 and increased the ratio of
Bax/Bcl-2 expression.
in vivo: chidamide in the dose range of 12.550 mg/kg dose-dependently reduced tumor size and tumor weight, and the dose of
50 mg/kg produced 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. Daily oral CS055 treatment of nude mice
bearing HL60 cell xenografts suppressed tumour growth, induced tumour cell apoptosis and prolonged the survival of
tumour-bearing mice.

Chemical Information
Catalog

DC7978

Purity of current batch:

>98%

Molecular Weight (MW)

390.41

Molecular Formula

C22H19FN4O2

CAS No.

743420-02-2

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in

advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.