1. TGF-beta/Smad
  2. TGF-β Receptor
  3. K02288

K02288 

Cat. No.: HY-12278 Purity: 99.66%
COA 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
Solution
10 mM * 1 mL in DMSO USD 196 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 196 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 178 In-stock
Estimated Time of Arrival: December 31
50 mg USD 594 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 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].

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

In Vivo

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

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

Molecular Weight

352.38

Formula

C20H20N2O4

CAS No.
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 available by MCE.
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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Product Name:
K02288
Cat. No.:
HY-12278
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