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  2. TGF-β Receptor
  3. K02288

K02288 

Cat. No.: HY-12278 Purity: 99.80%
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 IC50s of of 5-34 nM.

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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Based on 1 publication(s) in Google Scholar

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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 IC50s of of 5-34 nM.

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].

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.09 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.09 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.09 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

K02288K 02288K-02288TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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