Thi-DPPY

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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).

For research use only. We do not sell to patients.

Thi-DPPY Chemical Structure

CAS No. : 2307699-34-7

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

JAK3

1.38 nM (IC₅₀)

BTK

62.4 nM (IC₅₀)

In Vitro

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

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

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].

MedChemExpress (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.

Molecular Weight

566.07

Formula

C₂₈H₂₈ClN₅O₄S

CAS No.

2307699-34-7

SMILES

C=CC(NC1=CC(OC2=NC(NC3=CC(Cl)=C(C=C3)OCCCN4CCOCC4)=NC5=C2SC=C5)=CC=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhu Y, et al. Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis. Bioorg Med Chem. 2020 Jan 15;28(2):115254. [Content Brief]

Thi-DPPY Related Classifications

Molarity Calculator
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The molarity calculator equation

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

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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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