2. TGF-beta/Smad
  3. TGF-β Receptor
  4. TGFβ1-IN-2

TGFβ1-IN-2 is a diarylacylhydrazones derivative that effectively suppresses the activation and proliferation of fibroblasts. TGFβ1-IN-2 can be used for idiopathic pulmonary fibrosis (IPF) research.

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TGFβ1-IN-2 Chemical Structure

TGFβ1-IN-2 Chemical Structure

CAS No. : 2883813-66-7

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TGFβ1-IN-2 Related Antibodies

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Description

TGFβ1-IN-2 is a diarylacylhydrazones derivative that effectively suppresses the activation and proliferation of fibroblasts. TGFβ1-IN-2 can be used for idiopathic pulmonary fibrosis (IPF) research[1].

In Vitro

TGFβ1-IN-2 (compound 52) shows inhibitory effect against NIH-3T3 cells with an IC50 of 1.36 μM[1].
TGFβ1-IN-2 (compound 52; 6 μM; for 24 h) inhibits TGF-β1-induced abnormal activation of NIH-3T3 and A549 cells, as well as migration and epithelial-mesenchymal transition (EMT) of A549 cells[1].
TGFβ1-IN-2 (compound 52) could bind to STAT3, and able to interact with Ile659, and the hydrophilic group piperidine formed intermolecular forces with Ser636, Arg609, and Pro639[1].

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

TGFβ1-IN-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: NIH-3T3 or A549 cells
Concentration: 6 μM
Incubation Time: 24 h
Result: Were able to inhibit TGF-β1-induced activation of fibroblasts in vitro.
In Vivo

TGFβ1-IN-2 (compound 52; 30-60 mg/kg; p.o; once daily; for 22 days) improves mouse lung function and slowsthe progression of IPF. TGFβ1-IN-2 could reverse the pulmonary fibrosis in treatment model[1].
Pharmacokinetic parameters of TGFβ1-IN-2 (compound 52) in rats[1].

PK parameter TGFβ1-IN-2 (Compound 52)
i.v. p.o.
Dose (mg/kg) 2 20
Cmax (ng/mL) 470.58±60.67 351.01±85.44
Tmax (h) 0.08 2.17
AUC0-∞ (h·ng/mL) 370.81±76.46 1503.71±319.62
CL (mL/h/kg) 5565.86±1257.13 -
T1/2 (h) 0.93±0.43 1.23±0.15
F (%) - 42.08±8.93

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

Animal Model: C57BL/6 mice (6-10 weeks) injected with Bleomycin for establishing pulmonary fibrosis model[1].
Dosage: 30 mg/kg, 60 mg/kg
Administration: Orally administration; once daily; for 22 days
Result: Could reverse the pulmonary fibrosis in treatment model.
Molecular Weight

458.57

Formula

C23H30N4O4S
CAS No.
SMILES

O=C(C1=CC=C(C=C1)OCCCCCCN2CCCCC2)N/N=C/C3=CC=C(S3)[N+]([O-])=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
References
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TGFβ1-IN-2 Related Classifications

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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:

TGFβ1-IN-22883813-66-7TGF-β ReceptorTransforming growth factor beta receptorsTGF-β1diarylacylhydrazones derivativeidiopathic pulmonary fibrosisepithelial-mesenchymal transitionSTAT3Inhibitorinhibitorinhibit

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