Home TGF-beta/Smad TGF-beta/Smad inhibitor K02288 For research use only.

K02288

K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.

K02288 Chemical Structure

K02288 Chemical Structure

CAS No. 1431985-92-0

Purity & Quality Control

K02288 Related Products

Signaling Pathway

TGF-beta/Smad Signaling Pathways

TGF-beta/Smad Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C2C12 Function assay 30 mins Inhibition of BMP2-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay, IC50=0.23μM 25101911
C2C12 Function assay 30 mins Inhibition of BMP4-induced BMP receptor in mouse C2C12 cells after 30 mins by luciferase reporter gene assay, IC50=0.34μM 25101911
C2C12 Function assay 30 mins Inhibition of BMP6-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay, IC50=0.42μM 25101911
HEK293T Function assay 30 mins Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay, IC50=3.4μM 25101911
Click to View More Cell Line Experimental Data

Biological Activity

Description K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.
Features A chemical probe for BMP signaling in cells.
Targets
ALK2 [1]
(Cell-free assay)		 ALK1 [1]
(Cell-free assay)		 ALK6 [1]
(Cell-free assay)		 ALK3 [1]
(Cell-free assay)
1.1 nM 1.8 nM 6.4 nM 34.4 nM
In vitro
In vitro K02288 dose-dependently inhibits BMP4- and BMP6- induced Smad1/5/8 phosphorylation in C2C12 cells without affecting TGF-β-BMP signaling. [1]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-Smad1/5/8 / Smad1 p-Smad2 / Smad2 23646137
Growth inhibition assay Cell viability 23646137
In Vivo
In vivo In Zebrafish Embryos, K02288 induces a dorsalized phenotype in a dose dependent manner without effect om intersomitic vessel (ISV) formation. [1]
Animal Research Animal Models Zebrafish Embryos
Dosages ~10 µM
Administration --

Chemical Information & Solubility

Molecular Weight 352.38 Formula

C20H20N2O4
CAS No. 1431985-92-0 SDF Download K02288 SDF
Smiles COC1=CC(=CC(=C1OC)OC)C2=C(N=CC(=C2)C3=CC(=CC=C3)O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 70 mg/mL ( (198.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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