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199657-29-9

中文名稱 199657-29-9
英文名稱 Givinostat (hydrochloride)
CAS 199657-29-9
分子式 C24H28ClN3O4
分子量 457.95
MOL 文件 199657-29-9.mol
更新日期 2025/01/07 08:45:03
199657-29-9 結(jié)構(gòu)式 199657-29-9 結(jié)構(gòu)式

基本信息

中文別名
化合物 T6279L
化合物GIVINOSTAT HYDROCHLORIDE
英文別名
Givinostat Hcl
ITF-2357 hydrochloride
Gavinostat hydrochloride
Givinostat (ITF2357) HCl
Givinostat (hydrochloride)
Givinostat (ITF2357) hydrochloride
GAVINOSTAT HYDROCHLORIDE
ITF-2357 HYDROCHLORIDE
[6-[(Diethylamino)methyl]-2-naphthalenyl]methyl-N-[4-[(hydroxyamino)carbonyl]phenyl]carbamate hydrochloride
所屬類別
生物化工:激動劑抑制劑

物理化學性質(zhì)

儲存條件-20°C儲存
溶解度DMSO:45.8(Max Conc. mg/mL);100.01(Max Conc. mM)

常見問題列表

生物活性
Givinostat (ITF-2357) hydrochloride 是 HDAC 抑制劑,抑制 HDAC1 和 HDAC3,IC50 分別為 198 nM 和 157 nM。
靶點

hHDAC3

157 nM (IC 50 )

hHDAC1

198 nM (IC 50 )

hHDAC11

292 nM (IC 50 )

hHDAC6

315 nM (IC 50 )

hHDAC2

325 nM (IC 50 )

hHDAC10

340 nM (IC 50 )

hHDAC7

524 nM (IC 50 )

hHDAC5

532 nM (IC 50 )

hHDAC9

541 nM (IC 50 )

hHDAC8

854 nM (IC 50 )

hHDAC4

1059 nM (IC 50 )

HD1-B

7.5 nM (IC 50 )

HD1-A

16 nM (IC 50 )

HD2

10 nM (IC 50 )

體外研究

Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduces IL-1β secretion more than 70%. Givinostat suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 100 and 200 nM, there is no reduction. Givinostat (ITF-2357) inhibits JS-1 cell proliferation in a concentration-dependent manner in the CCK-8 assay. Treatment with Givinostat (ITF-2357) ≥500 nM is associated with significant inhibition of JS-1 cell proliferation. Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat (ITF-2357) ≥250 nM plus LPS and the group without LPS treatment.

體內(nèi)研究

Givinostat (ITF2357) at 10 mg/kg is used as a positive control and reduces serum TNFα by 60%. Pretreatment of Givinostat (ITF-2357) starting at 0.1 mg/kg significantly reduces the circulating TNFα by nearly 90%. To achieve a significant increase in serum IL-1β production, a higher dose of LPS is injected (10 mg/kg), and blood is collected after 4 h.

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