HDAC1-IN-3

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HDAC1-IN-3

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

HDAC1-IN-3 是一种有效的Pf HDAC1抑制剂。HDAC1-IN-3 在野生型和耐多药寄生虫菌株中均显示出抗疟活性。HDAC1-IN-3 对寄生虫所有生命周期显示出显著的体内杀伤作用。

生物活性

HDAC1-IN-3 is a potentPfHDAC1inhibitor. HDAC1-IN-3 shows antimalarial activity in wild-type and multidrug-resistantparasitestrains. HDAC1-IN-3 shows a significant in vivo killing effect against all life cycles of parasites^[1].

IC₅₀& Target

HDAC1

2.2 nM (IC₅₀)

HDAC2

5.1 nM (IC₅₀)

HDAC3

5.2 nM (IC₅₀)

HDAC6

85.5 nM (IC₅₀)

HDAC8

29.9 nM (IC₅₀)

Plasmodium

体外研究
(In Vitro)

HDAC1-IN-3 (compound JX35) shows antimalarial activity with IC₅₀s of 1.26 nM and 1.61 nM for wild-typePlasmodium falciparum (P. falciparum)parasite 3D7 and chloroquine-resistantP. falciparumparasite Dd2, respectively^[1].
HDAC1-IN-3 (10 μM; 72 h) shows low cytotoxicity with IC₅₀s of 1.02 μM and 1.21 μM for HepG2, 293T cells, respectively^[1].
HDAC1-IN-3 (72 h) shows no cross-resistance with clinical antimalarial drugs with IC₅₀s of 3.06, 2.18, 5.85 nM for GB4, C2A, CP286, respectively^[1].
HDAC1-IN-3 (10, 30, 60, 100 nM; 3, 6, 12, 24 h) shows antimalarial activity in a time- and dose-dependent manner with asynchronous 3D7 parasites^[1].
HDAC1-IN-3 (40 nM, 4 days;P. falciparum3D7 cells) shows the killing effects of JX35 onP. falciparumparasites during asexual reproduction stages might be related to the inhibition of schizont growth and reinvasion of RBCs (red blood cells)^[1].
HDAC1-IN-3 (5, 20 nM; 4 h) inhibits the expression of Pf HDAC against ART (artemisinin)-resistant parasite strains^[1].
HDAC1-IN-3 reduces the inhibition of hHDACs with IC₅₀s of 2.2, 5.1, 5.2, 85.5, 29.9 nM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively^[1].

Cell Cytotoxicity Assay^[1]

Cell Line:	HepG2, 293T cells
Concentration:	10 μM
Incubation Time:	72 h
Result:	Showed low cytotoxicity with IC₅₀s of 1.02 μM and 1.21 μM for HepG2, 293T cells, respectively.

Western Blot Analysis^[1]

Cell Line:	P. falciparum3D7 cells
Concentration:	5, 20 nM
Incubation Time:	4 h
Result:	Inhibited the expression of Pf HDAC against ART (artemisinin)-resistant parasite strains.

体内研究
(In Vivo)

HDAC1-IN-3 (30, 60, 90 mg/kg; i.p.; once daily for 5 days) shows acceptable therapeutic efficacy and safety^[1].
HDAC1-IN-3 (5 mg/kg; i.p.) shows good pharmacokinetic properties^[1].
Pharmacokinetic Parameters of HDAC1-IN-3 in Female BALB/c mice^[1].

parameter	JX35
C_max(ng/mL)	539
T_max(h)	0.25
AUC_last(h·ng/mL)	638
AUC_inf(h·ng/mL)	640
t_1/2(h)	0.91
CL_Z/F(L/h/kg)	7.81
V_Z/F(L/kg)	10.20

Female BALB/c mice; 5 mg/kg; i.p.

Animal Model:	6-8 weeks, BALB/c female mice^[1]
Dosage:	30, 60, 90 mg/kg
Administration:	I.p., once daily for 5 days
Result:	Showed acceptable therapeutic efficacy and safety.

Animal Model:	6-8 weeks, female BALB/c mice^[1]
Dosage:	5 mg/kg
Administration:	I.p.
Result:	Showed good pharmacokinetic properties.

分子量

453.92

Formula

C₂₂H₂₄ClN₇O₂

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.