2. TGF-beta/Smad
  3. TGF-β Receptor
  4. AZ12799734

AZ12799734 

Cat. No.: HY-123900
Handling Instructions

AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor.

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

AZ12799734 Chemical Structure

AZ12799734 Chemical Structure

CAS No. : 1117684-36-2

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Description

AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor[1].

IC50 & Target

TGFBR1

47 nM (IC50)

ALK6

0.017 μM (Kd)

ALK5

0.74 μM (Kd)

ALK4

1 μM (Kd)

ACVR1

6.2 μM (Kd)

ALK1

7.1 μM (Kd)

BMPR1A

40 μM (Kd)

BMP

 

In Vitro

AZ12799734 inhibits ligand activated SMAD3/4 transcription[1].
AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2[1].
AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells[1].

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

Western Blot Analysis[1]

Cell Line: HaCaT cells and NIH3T3 cells
Concentration: 10 nM
Incubation Time: 10 days (HaCaT) or 24 h (NIH3T3)
Result: Blocked TGFβ-mediated induction of SMAD2 phosphorylation. Inhibited phosphorylation of both SMAD1 and SMAD2.

Cell Migration Assay [1]

Cell Line: HaCaT epithelial cells
Concentration: 500 nM
Incubation Time: 36 h
Result: A dose-dependent decrease in TGFβ-induced migration was observed.
In Vivo

AZ12799734 (0-400 mg/kg/day; p.o.; 3-7 days) induces histopathologic heart valve lesions in rat[2].
AZ12799734 (50 mg/kg; p.o.; once) shows total and free pharmacokinetic (PK) levels in the nude mouse with time over in vitro IC50 of 0.01885 μM[1].

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

Animal Model: Ten-week-old female HsdHan:WIST rats[2]
Dosage: 200 and 400 mg/kg/day
Administration: Oral, 3-7 days
Result: Hemorrhage into the heart valves was evident at low magnification and the normal architecture of the leaflet was replaced by hemorrhage.
Increased valvular interstitial cells in size and number and shows increased cytoplasm, an enlarged round to spindeloid nucleus, and frequently undergoing mitosis.
Animal Model: Female BALB/c mice[1]
Dosage: 50 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: Showed total and free pharmacokinetic (PK) levels with time over in vitro IC50 of 0.01885 μM.
Molecular Weight

370.43

Formula

C18H18N4O3S
CAS No.
SMILES

O=S(C1=CC=C(NC2=NC=CC(OC3=CC=C(C)N=C3C)=C2)C=C1)(N)=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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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.

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Keywords:

AZ127997341117684-36-2AZ 12799734AZ-12799734TGF-β ReceptorTransforming growth factor beta receptorsHaCaTSMAD1SMAD2SMAD3/4TGFBR1BMPheart valve lesionsInhibitorinhibitorinhibit

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