2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Cell Cycle/DNA Damage Apoptosis
  3. JAK HDAC Apoptosis
  4. JAK/HDAC-IN-2

JAK/HDAC-IN-2 是一种有效的 JAK/HDAC 双靶点抑制剂。JAK/HDAC-IN-2 在纳摩尔水平上有效抑制 HDAC3/6 和 JAK1/2。JAK/HDAC-IN-2 具有促凋亡活性，并抑制组蛋白去乙酰化和 STAT3 磷酸化。JAK/HDAC-IN-2 在血液恶性肿瘤和实体癌中均具有显着的抗增殖活性。

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JAK/HDAC-IN-2 Chemical Structure

JAK/HDAC-IN-2 Chemical Structure

CAS No. : 3029138-43-7

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JAK/HDAC-IN-2 相关抗体

Top Publications Citing Use of Products

查看 JAK 亚型特异性产品:

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JAK1 JAK2 JAK3 Tyk2 JAK

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers[1].

IC50 & Target[1]

JAK2

5.32 nM (IC50)

JAK1

27.15 nM (IC50)

JAK3

594.8 nM (IC50)

Tyk2

414.4 nM (IC50)

HDAC

170 nM (IC50)

HDAC1

340 nM (IC50)

HDAC2

303 nM (IC50)

HDAC3

58.7 nM (IC50)

HDAC6

4.44 nM (IC50)

HDAC10

116.1 nM (IC50)

HDAC11

724.4 nM (IC50)

HDAC4

>10000 nM (IC50)

HDAC5

>10000 nM (IC50)

HDAC7

>10000 nM (IC50)

HDAC8

>10000 nM (IC50)

HDAC9

>10000 nM (IC50)

体外研究
(In Vitro)

JAK/HDAC-IN-2 (化合物 21) 对 K562、HL-60 和 HEL 细胞表现出很强的抗增殖活性 (IC50 分别为 1.87、2.26 和 0.33 μM)；抑制四种实体瘤细胞 MCF-7、HeLa、A549 和 PC-3 的增殖 (IC50 分别为 1.83、2.88、0.73 和 2.52 μM)[1]。
JAK/HDAC-IN-2 (1, 5 μM; 24 小时) 在 HEL 细胞中具有优异的促凋亡活性，在 A549 细胞中具有中等的促凋亡活性[1]。
JAK/HDAC-IN-2 (1, 5 μM; 24 小时) 通过抑制 HDAC 和 JAK，显着抑制血液恶性肿瘤 HEL 细胞以及实体瘤 A549 细胞中的组蛋白去乙酰化和 STAT3 磷酸化[1]。

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

JAK/HDAC-IN-2 相关抗体:

Apoptosis Analysis[1]

Cell Line: HEL cells
Concentration: 1, 5 μM
Incubation Time: 24 h
Result: The apoptotic rates were 37.6% at 1 μM and 81.5% at 5 μM on HEL cells.

Western Blot Analysis[1]

Cell Line: A549 and HEL cells
Concentration: 1, 5 μM
Incubation Time: 24 h
Result: Bviously upgraded the expression level of acetyl-H3 and acetyl-tubulin in A549 cells in a dose-dependent manner.
Reduced the expression level of p-STAT3-Tyr705.
体内研究
(In Vivo)

JAK/HDAC-IN-2 (化合物 21; 50 mg/kg; 腹膜内注射; 每天一次; 连续 18 天) 在体内对血液恶性肿瘤 HEL 和实体瘤 A549 中表现出有效的抗肿瘤活性[1]。
Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats[1].

IV (3 mg/kg) PO (15 mg/kg)
Tmax (h) 2.912
Cmax (ng/mL) 93.328
AUC0-t (ng/mL∗h) 656.241 745.249
t1/2 (h) 0.128 2.084
CL (L/ kg∗h) 4.571 4.56
Vss (L/kg) 0.845
F (%) 22.71%

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

Animal Model: C57BL/6 nude mice[1]
Dosage: 50 mg/kg
Administration: Intraperitoneally; once a day for 18 consecutive days
Result: Prominently reduced the weight and volume of HEL and A549 xenografts.
Upgraded the expression level of acetyl-H3 as well as acetyl-tubulin and reduced the expression level of p-STAT3-Tyr705 in HEL as well as A549 xenograft tumor tissues.
分子量

570.70

Formula

C28H38N6O5S
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

JAK/HDAC-IN-2 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:

JAK/HDAC-IN-23029138-43-7JAKHDACApoptosisJanus kinaseHistone deacetylases2-amino-4-phenylaminopyrimidineJAK/HDACHDAC3HDAC6JAK1/2histone deacetylationSTAT3 phosphorylationhematological malignanciessolid cancersK562HL-60HELMCF-7HeLaA549PC-3Inhibitorinhibitorinhibit

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