2. TGF-beta/Smad MAPK/ERK Pathway
  3. TGF-β Receptor p38 MAPK
  4. J-1149

J-1149 is a potent ALK5 inhibitor, with an IC50 value of 0.017 μM. J-1149 also shows weak p38α MAP kinase inhibitory activity, with an IC50 value of 0.435 μM. J-1149 can be used for liver fibrosis research.

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

J-1149 Chemical Structure

J-1149 Chemical Structure

CAS No. : 2883580-95-6

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J-1149 Related Antibodies

Top Publications Citing Use of Products

View All TGF-β Receptor Isoform Specific Products:

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

View All p38 MAPK Isoform Specific Products:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • Biological Activity

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Description

J-1149 is a potent ALK5 inhibitor, with an IC50 value of 0.017 μM. J-1149 also shows weak p38α MAP kinase inhibitory activity, with an IC50 value of 0.435 μM. J-1149 can be used for liver fibrosis research[1].

IC50 & Target

ALK5

0.017 μM (IC50)

p38α MAPK

 

In Vitro

J-1149 (compound 15g) (5-40 μM, 24 h) efficiently inhibits extracellular matrix (ECM) deposition in TGF-β-induced hepatic stellate cells (HSCs), and eventually suppresses HSC activation[1].
J-1149 (20 μM, 24 h) inhibits the expression of α-SMA and collagen I stimulated by TGF-β[1].

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

J-1149 Related Antibodies

Western Blot Analysis[1]

Cell Line: LX-2 cells
Concentration: 20 μM
Incubation Time: 1 h prior to TGF-β stimulation for continuous 24 h
Result: Inhibited the expression of α-SMA and collagen I stimulated by TGF-β.
In Vivo

J-1149 (compound 15g) shows a good pharmacokinetic (PK) profile with a favorable half-life (t1/2 = 9.14 h)[1].

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

Animal Model: Sprague Dawley (SD) rats[1]
Dosage: 4 mg/kg (IV), 15 mg/kg (PO)
Administration: IV or PO, once (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of J-1149 in male Sprague-Dawley rats[1].
IV (4 mg/kg) PO (15 mg/kg)
Tmax (h) 0.00 ± 0.00 0.11 ± 0.13
Cmax (ng/mL) 43,144 ± 35,001 1386 ± 882
AUC0-t (ng/mL∗h) 12,529 ± 978 1217 ± 20
AUC0-∞ (ng/mL∗h) 12,802 ± 1160 2667 ± 1136
t1/2 (h) 2.24 ± 1.05 9.14 ± 5.13
CL (mL/h/kg) 314 ± 28 6564 ± 3372
F (%) 2.59%
Molecular Weight

452.51

Formula

C25H24N8O
CAS No.
SMILES

N[C@H](CC1=CC=CC=C1)C(NCC2=NC(C3=CC=CC(C)=N3)=C(C4=CN5C(C=C4)=NC=N5)N2)=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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J-1149 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:

J-11492883580-95-6J1149J 1149TGF-β Receptorp38 MAPKTransforming growth factor beta receptorsTGF-βα-SMAcollagen ILX-2 cellsliver fibrosishepatic stellate cellsInhibitorinhibitorinhibit

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