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RepSox (E-616452) TGF-beta/Smad inhibitor

Cat.No.S7223

RepSox (E-616452, SJN 2511, ALK5 Inhibitor II) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively.

RepSox (E-616452) TGF-beta/Smad inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 287.32

Quality Control

Batch: Purity: 99.92%

99.92

Related Targets	PKC ROCK Bcr-Abl
Other TGF-beta/Smad Inhibitors	SB431542 Vactosertib (TEW-7197) LDN-193189 A-83-01 LDN-193189 Dihydrochloride Galunisertib (LY2157299) SRI-011381 (C381) LY2109761 SIS3 Hydrochloride SB-525334

Solubility in DMSO or Water

In vitro
Batch:

DMSO : 57 mg/mL (198.38 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 57 mg/mL (198.38 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 57 mg/mL (198.38 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 57 mg/mL (198.38 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 57 mg/mL (198.38 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.

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.

Read more about RepSox (E-616452) solubility in DMSO or water

Working Concentrations for Cell Culture Treatment

Read more about RepSox (E-616452) working concentrations for cell culture treatment

Working Concentrations for Animal Model Treatment

Mechanism of Action

Information	RepSox (E-616452) is a potent TGF-βR1 (ALK5) inhibitor. It affects the TGF-β/Smad signaling pathway, and by blocking Smad2/3 phosphorylation, it promotes cellular reprogramming, pluripotency, and inhibits epithelial-mesenchymal transition (EMT).
Read more about RepSox (E-616452) IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Read more about RepSox (E-616452) Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	287.32	Formula	C₁₇H₁₃N₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	446859-33-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SJN 2511,ALK5 Inhibitor II			Smiles	CC1=NC(=CC=C1)C2=C(C=NN2)C3=NC4=C(C=C3)N=CC=C4

Read more about storage & stability

RepSox (E-616452) VS A-83-01 | SB431542 | Galunisertib (LY2157299)

Read more comparative analysis about RepSox (E-616452)

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions

Concentration (start):

Dilution-folds:

Computed Result

C1=C0/X	C1:		LOG(C1):
C2=C1/X	C2:		LOG(C2):
C3=C2/X	C3:		LOG(C3):
C4=C3/X	C4:		LOG(C4):
C5=C4/X	C5:		LOG(C5):
C6=C5/X	C6:		LOG(C6):
C7=C6/X	C7:		LOG(C7):
C8=C7/X	C8:		LOG(C8):