2. Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. Apoptosis HDAC
  4. HDAC-IN-31

HDAC-IN-31 是一种有效、选择性和具有口服活性的 HDAC 抑制剂，HDAC1、HDAC2、HDAC3、HDAC8 的 IC50 值分别为 84.90, 168.0, 442.7, >10000 nM。 HDAC-IN-31 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在在 G2/M 期。HDAC-IN-31 显示出良好的抗肿瘤功效。HDAC-IN-31 具有研究弥漫性大B细胞淋巴瘤的潜力。

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HDAC-IN-31 Chemical Structure

HDAC-IN-31 Chemical Structure

CAS No. : 1916505-13-9

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HDAC-IN-31 相关抗体

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-31 is a potent, selective and orally active HDAC inhibitor with IC50s of 84.90, 168.0, 442.7, >10000 nM for HDAC1, HDAC2, HDAC3, HDAC8, respectively. HDAC-IN-31 induces apoptosis and cell cycle arrests at G2/M phase. HDAC-IN-31 shows good antitumor efficacy. HDAC-IN-31 has the potential for the research of diffuse large B-cell lymphoma[1].

IC50 & Target[1]

HDAC1

84.90 nM (IC50)

HDAC2

168.0 nM (IC50)

HDAC3

442.7 nM (IC50)

HDAC8

>10000 nM (IC50)

体外研究
(In Vitro)

HDAC-IN-31 (compound 24g) (2 µM) shows growth-inhibitory activities with the inhibition rate of 2.32%, 44.01%, 48.53%, 64.94% for TMD-8, HCT 116, A549, MDA-MB-231 cells[1].
HDAC-IN-31 (1 µM) shows selectivity with the IC50s of 84.9, 168.0, 442.7, >10000 nM for HDAC 1, HDAC 2, HDAC 3, HDAC 8, and 81.20%, 84.43%, 88.07%, 92.34%, 96.88%, 91.98% enzyme activity for HDAC4, HDAC 5,HDAC 7, HDAC9, HDAC 6, HDAC 11, respectively[1].
HDAC-IN-31 (2.5, 5, 7.5, 10 µM; 24 h) increases the expression of HDAC1, Ace-H3, Ace-H4, Cleaved PARP, Cleaved Caspase-3 in a dose-dependent manner[1].
HDAC-IN-31 (0-4 µM; 24 h)induce apoptosis and cell cycle arrests in G2/M phase in a dose-dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

HDAC-IN-31 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, A549, NCI-H460, HCT-116,SK-OV-3, HT-29, COLO 678, NCI-H441, 22Rv1, 786-O, TMD-8, DOHH-2, CCRF-CEM, SU-DHL-2, REC-1, MOLT-4, HUT-78, RS4;11 cells
Concentration: 0-20 µM
Incubation Time: 72 h
Result: Showed a broad spectrum of antitumor activity with the IC50s of 2.29, 2.85, 1.58, 1.16, 3.17, 2.41, 8.02, 2.62, 1.14, 0.60, 0.31, 0.39, 0.48, 0.51, 0.33, 0.38, 0.80, 0.47 µM for MDA-MB-231, A549, NCI-H460, HCT-116, SK-OV-3, HT-29, COLO 678, NCI-H441, 22Rv1, 786-O, TMD-8, DOHH-2, CCRF-CEM, SU-DHL-2, REC-1, MOLT-4, HUT-78, RS4;11 cells, respectively.

Western Blot Analysis[1]

Cell Line: TMD-8 cells
Concentration: 2.5, 5, 7.5, 10 µM
Incubation Time: 24 h
Result: Promoted the HDAC1, HDAC2, HDAC3 substrate Ace-H3 and Ace-H4 acetylation with a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: TMD-8 cells
Concentration: 0.5, 1, 2, 4 µM
Incubation Time: 24 h
Result: Induced cell apoptosis at a concentration-dependent manner.

Cell Cycle Analysis[1]

Cell Line: TMD-8 cells
Concentration: 250, 500, 1000 nM
Incubation Time: 24 h
Result: Arrested the cell cycle at G2/M phase in a dose-dependent manner.
体内研究
(In Vivo)

HDAC-IN-31 (2 mg/kg for i.v.; 10, 100 mg/kg for p.o.) shows good bioavailability with a significant dose dependent manner[1].
HDAC-IN-31 (50, 100 mg/kg; p.o, daily for 21 consecutive days) shows good antitumor efficacy in a TMD-8 xenograft model without obvious toxicity[1].
Pharmacokinetic Parameters of HDAC-IN-31 in mice[1].

Parameters Unit 24 g (25 mg/kg)
Cmax ng·h·mL-1 3100±231
T1/2(po) h 4.4±0.3
AUC0-inf(iv) ng·h·mL-1 1040±142
AUC0-inf(po) ng·h·mL-1 5180±252
MRTPO h 2.6±0.4
F % 39.9±2.1
ICR mouse; 2 mg/kg for i.v.; 25 mg/kg for p.o.[1].
Pharmacokinetic Parameters of HDAC-IN-31 in tumor models[1].
Parameters Unit po (25 mg/kg) po (50 mg/kg) po (100 mg/kg)
Cmax ng·h·mL-1 1700±317 14700±1024 10700±1001
AUC0-t ng·h·mL-1 1220±242 9710±314 9740±230
AUC0-inf ng·h·mL-1 1230±165 9730±341 9770±332
MRT0-t h 0.750±0.043 0.812±0.023 1.43±0.56
MRT0-inf h 0.805±0.086 0.821±0.041 1.51±0.32
Mouse; 25, 50, 100 mg/kg for p.o.[1].
Pharmacokinetic Parameters of HDAC-IN-31 in tumor models[1].
PK parameters Unit iv (2 mg/kg) po (10 mg/kg) po (100 mg/kg)
Cmax ng·h·mL-1 3960±413 58300±1352
T1/2 h 0.427±0.016 1.31±0.27 1.63±0.52
AUC0-inf ng·h·mL-1 1250±132 2670±286 57200±1047
MRT h 0.402±0.032 0.919±0.052 0.897±0.041
CL mL·kg·min-1 27.2±1.2
F % 45.6±1.2 91.8±2.3
ICR mice; 2 mg/kg for i.v.; 10, 100 mg/kg for p.o.[1].
Pharmacokinetic Parameters of HDAC-IN-31 in tumor models[1].
PK parameters Unit Monkey Dog
iv (1 mg/kg) po (10 mg/kg) iv (1 mg/kg) po (10 mg/kg)
Cmax ng·h·mL-1 8520±301 4740±243
T1/2 h 4.31±0.56 9.14±0.32 1.65±0.41 1.51±0.33
AUC0-inf ng·h·mL-1 15700±1842 53200±1241 2550±365 15100±2004
MRT h 3.41±0.12 8.28±0.32 2.26±0.41 2.71±0.32
CL mL·kg·min-1 1.35±0.21 6.72±0.35
Vdss L·kg-1 0.34±0.22 0.55±0.04
F % 27.6±2.1 58.9±1.2
Dogs and monkeys; 1 mg/kg for i.v., 10 mg/kg for p.o. for monkey; 1 mg/kg for i.v., 10 mg/kg for p.o. for dog[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR mice[1]
Dosage: 2 mg/kg for i.v.; 25 mg/kg for p.o.(DMSO/PEG200/saline = 20:20:60, v/v/v)
Administration: I.v. or p.o.
Result: Showed high oral bioavailability (F=40%).
Animal Model: Mouse[1]
Dosage: 25, 50, 100 mg/kg
Administration: P.o.
Result: Did not exhibit a significant dose dependent for oral administration.
Animal Model: ICR mice[1]
Dosage: 2, 10, 100 mg/kg (into the form of hydrochloride)
Administration: 2 mg/kg for i.v.; 10, 100 mg/kg for p.o.
Result: Showed good bioavailability with a significant dose dependent.
Animal Model: Dogs and monkeys[1]
Dosage: 1, 10 mg/kg
Administration: 1 mg/kg for i.v.; 10 mg/kg for p.o.
Result: Showed good pharmacokinetic characteristics for different species.
Animal Model: 5-6 weeks, female CB.17 SCID mice (TMD-8 tumor xenografts)[1]
Dosage: 50, 100 mg/kg
Administration: P.o, daily for 21 consecutive days
Result: Inhibited the tumor growth with the inhibition rate of 77% and had no significant effect on the internal organs of mice at 100 mg/kg/d.
分子量

412.48

Formula

C25H24N4O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

HDAC-IN-31 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

HDAC-IN-311916505-13-9ApoptosisHDACHistone deacetylasesdiffuse large B-cell lymphomaantitumorselectiveorally activeG2/MTMD-8 tumor xenograftsInhibitorinhibitorinhibit

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