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.
For research use only. We do not sell to patients.
- CAS No.: 2883813-66-7
- Formula: C23H30N4O4S
- Molecular Weight:458.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | IC50 |
1.36 μM
Compound: 52
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Antiproliferative activity against NIH3T3 cells after 72 hrs by MTT assay
Antiproliferative activity against NIH3T3 cells after 72 hrs by MTT assay
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[PMID: 36401884] |
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.
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Cell Line:NIH-3T3 or A549 cells
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Concentration:6 μM
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Incubation Time:24 h
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Result:Were able to inhibit TGF-β1-induced activation of fibroblasts in vitro.
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.
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Animal Model:C57BL/6 mice (6-10 weeks) injected with Bleomycin for establishing pulmonary fibrosis model[1].
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Dosage:30 mg/kg, 60 mg/kg
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Administration:Orally administration; once daily; for 22 days
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Result:Could reverse the pulmonary fibrosis in treatment model.
Chemical Information
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CAS No. 2883813-66-7
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Molecular Weight 458.57
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Formula C23H30N4O4S
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SMILES
O=C(C1=CC=C(C=C1)OCCCCCCN2CCCCC2)N/N=C/C3=CC=C(S3)[N+]([O-])=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TGFβ1-IN-2 Related Classifications
HY-151954 Related Classifications
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