1. TGF-beta/Smad
    Protein Tyrosine Kinase/RTK
  2. TGF-β Receptor
    ALK

K02288 

Cat. No.: HY-12278 Purity: 99.43%
Handling Instructions

K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50

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

K02288 Chemical Structure

K02288 Chemical Structure

CAS No. : 1431985-92-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 178 In-stock
Estimated Time of Arrival: December 31
10 mg USD 162 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50

IC50 & Target

IC50:1.8 nM (ALK1), 1.1 nM (ALK2), 34.4 nM (ALK3), 6.3 nM (ALK6), 302 nM (ALK4), 321 nM (ALK5)[1]

In Vitro

K02288 reduces a robust phosphorylation of Smad1/5/8 induced by BMP4 stimulation, with an apparent IC50 of 100 nM. K02288 causes near complete inhibition of Smad2 phosphorylation at 0.5 µM[1]. K02288 binds to ALK1 in an ATP-mimetic fashion with two hydrogen bonds to the kinase hinge. K02288 also inhibits BMP9-ALK1 signalling, and induces a hypersprouting phenotype in HUVECs[2].

In Vivo

K02288 (1 µM) induces dysfunctional angiogenesis in a chick embryo CAM model[2].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 58.6 mg/mL (166.30 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8378 mL 14.1892 mL 28.3785 mL
5 mM 0.5676 mL 2.8378 mL 5.6757 mL
10 mM 0.2838 mL 1.4189 mL 2.8378 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

352.38

Formula

C₂₀H₂₀N₂O₄

CAS No.

1431985-92-0

SMILES

OC1=CC=CC(C2=CC(C3=CC(OC)=C(OC)C(OC)=C3)=C(N)N=C2)=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
K02288
Cat. No.:
HY-12278
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K02288

Cat. No.: HY-12278