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K02288 TGF-beta/Smad inhibitor

Name: K02288
Brand: Selleck Chemicals
SKU: S7359
Availability: InStock
Rating: 5 (24 reviews)

Cat.No.S7359

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.

Chemical Structure

Molecular Weight: 352.38

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.84%

99.84

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Chemical Information, Storage & Stability

Molecular Weight	352.38	Formula	C₂₀H₂₀N₂O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1431985-92-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	COC1=CC(=CC(=C1OC)OC)C2=C(N=CC(=C2)C3=CC(=CC=C3)O)N

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (198.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Mechanism of Action

Features	A chemical probe for BMP signaling in cells.
Targets/IC₅₀/Ki	ALK2 ^[1] (Cell-free assay) 1.1 nM ALK1 ^[1] (Cell-free assay) 1.8 nM ALK6 ^[1] (Cell-free assay) 6.4 nM ALK3 ^[1] (Cell-free assay) 34.4 nM
In vitro	K02288 dose-dependently inhibits BMP4- and BMP6- induced Smad1/5/8 phosphorylation in C2C12 cells without affecting TGF-β-BMP signaling. ^[1]
In vivo	In Zebrafish Embryos, K02288 induces a dorsalized phenotype in a dose dependent manner without effect om intersomitic vessel (ISV) formation. ^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/23646137/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-Smad1/5/8 / Smad1 p-Smad2 / Smad2		23646137
Growth inhibition assay	Cell viability		23646137

Tech Support

Handling Instructions

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