2. Cell Cycle/DNA Damage Epigenetics Anti-infection
  3. HDAC Parasite
  4. HDAC1-IN-3

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。

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HDAC1-IN-3 Chemical Structure

HDAC1-IN-3 Chemical Structure

CAS No. : 2482998-35-4

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HDAC1-IN-3 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

查看 Parasite 亚型特异性产品:

查看所有亚型
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC1-IN-3 is a potent Pf HDAC1 inhibitor. HDAC1-IN-3 shows antimalarial activity in wild-type and multidrug-resistant parasite strains. 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-type Plasmodium falciparum (P. falciparum) parasite 3D7 and chloroquine-resistant P. falciparum parasite 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. falciparum 3D7 cells) shows the killing effects of JX35 on P. falciparum parasites 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].

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

HDAC1-IN-3 相关抗体:

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. falciparum 3D7 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
Cmax (ng/mL) 539
Tmax (h) 0.25
AUC last (h·ng/mL) 638
AUC inf (h·ng/mL) 640
t1/2 (h) 0.91
CLZ/F (L/h/kg) 7.81
VZ/F (L/kg) 10.20
Female BALB/c mice; 5 mg/kg; i.p.

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

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
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

HDAC1-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HDAC1-IN-32482998-35-4HDACParasiteHistone deacetylasesAntimalarialchloroquine-resistantP. falciparum 3D7 cellslife cyclesadequate safetymultidrug-resistantfemale micelow toxicityInhibitorinhibitorinhibit

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