2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  3. JAK
  4. Thi-DPPY

Thi-DPPY (compound 8e) 是一种有效且具有口服活性的 JAK3 抑制剂，对 BTK、JAK 的 IC50 值分别为62.4, 1.38 nM。Thi-DPPY 对 HBE 细胞具有抗增殖活性。Thi-DPPY 在体内显示出抗炎活性。Thi-DPPY 具有研究特发性肺纤维化（IPF）的潜力。

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Thi-DPPY Chemical Structure

Thi-DPPY Chemical Structure

CAS No. : 2307699-34-7

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Thi-DPPY 相关抗体

Top Publications Citing Use of Products

查看 JAK 亚型特异性产品:

查看所有亚型
JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF)[1].

IC50 & Target[1]

JAK3

1.38 nM (IC50)

BTK

62.4 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Sf9 IC50
1.38 nM
Compound: 8e
Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay
Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay
[PMID: 31866272]
体外研究
(In Vitro)

DPPY (compound 8e) shows anti-proliferative activity against HBE (human bronchial epithelia) cells with an IC50 of 39.0 µM[1].

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

Thi-DPPY 相关抗体:
体内研究
(In Vivo)

DPPY (30, 60 mg/kg; i.g., once daily for 14 days) shows anti-IPF agents on the lung morphology and lung coefficient in mouse model[1].
DPPY (30, 60 mg/kg) significantly decreases the expression of IL-6, IL-17A, TNF-α and MDA in lung tissue in a dose dependent manner[1].

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

Animal Model: 5-6 week old, 20-25 g, C57BL mice (BLM-induced pulmonary inflammation and pulmonary fibrosis model)[1]
Dosage: 30, 60 mg/kg
Administration: I.g.; once daily for 14 days
Result: Attenuated the pulmonary morphology changes and reduced the collagen disposition induced by BLM in mouse lung.
分子量

566.07

Formula

C28H28ClN5O4S
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

Thi-DPPY 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:

Thi-DPPY2307699-34-7JAKJanus kinaseidiopathic pulmonary fibrosis,HBE cellsanti-proliferativeanti-inflammatoryIL-6IL-17ATNF-αBLM-induced pulmonary inflammationInhibitorinhibitorinhibit

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