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RepSox (ALK5 Inhibitor II)

Cat. No. M1859
RepSox (ALK5 Inhibitor II) Structure

RepSox; E-616452; SJN 2511

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 100 In stock
25mg USD 200 In stock
50mg USD 350 In stock
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Quality Control
Biological Activity

ALK5 Inhibitor (RepSox) is a potent and selective inhibitor of the TGF-β RI kinase with IC50 values of 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding, respectively. It enhances the efficiency of cellular reprogramming. ALK5 Inhibitor affects a range of related kinases selectively, including p38 MAPK, GSK3 and JNK1 (IC50 > 16 μM).

Customer Product Validations & Biological Datas
Source PLoS One (2013). Figure 3. ALK5 Inhibitor II
Method HSA staining
Cell Lines HepG2 and HSC cells
Concentrations 10 μM
Incubation Time 48 h
Results The specificity of the conjugate was also determined by examining the effect of both free LY364947 and conjugate on HepG2 hepatocytes. The conjugate did not bind to these cells
Source PLoS One (2013). Figure 2. ALK5 Inhibitor II
Cell Lines HepG2 and HSC cells
Concentrations 10 μM
Incubation Time 48 h
Results Both free LY-364947 and the conjugate significantly inhibited TGF-b1-induced Smad signaling, measured as luciferase activity, whereas the carrier itself did not have any effect.
Cell Experiment
Cell lines iPS cells
Preparation method Cell Cyle Analysis Cells were treated with 25 μΜ RepSox in mES media without feeders for 72 hours and subjected to cell cycle analysis by propidium iodide staining and flow cytometry. Cells were harvested with .25% trypsin and fixed with 70% ethanol overnight. Following at least one hour of incubation with propidium iodide staining solution (50 μg/ml propidium iodide in PBS, .1% BSA, .1% Rnase A) in the dark, samples were analyzed on a BD LRSII Flow Cytometer (BD Biosciences).
Concentrations 25µM
Incubation time 72 h
Animal Experiment
Animal models chimeric embryos E13.5
Formulation not refered
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 287.32
Formula C17H13N5
CAS Number 446859-33-2
Purity 99.67%
Solubility DMSO ≥ 50 mg/mL
Storage at -20°C

Cotreatment with RepSox and LBH589 improves the invitro developmental competence of porcine somatic cell nuclear transfer embryos.
Luo ZB, et al. Reprod Fertil Dev. 2018 Apr 24. PMID: 29685182.

Transforming growth factor β-inhibitor Repsox downregulates collagen expression of scleroderma dermal fibroblasts and prevents bleomycin-induced mice skin fibrosis.
Ide M, et al. Exp Dermatol. 2017 Nov;26(11):1139-1143. PMID: 28418584.

RepSox improves viability and regulates gene expression in rhesus monkey-pig interspecies cloned embryos.
Zhu HY, et al. Biotechnol Lett. 2017 May;39(5):775-783. PMID: 28247195.

A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog.
Ichida JK, et al. Cell Stem Cell. 2009 Nov 6;5(5):491-503. PMID: 19818703.

Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
Gellibert F, et al. J Med Chem. 2004 Aug 26;47(18):4494-506. PMID: 15317461.

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Keywords: RepSox (ALK5 Inhibitor II), RepSox; E-616452; SJN 2511 supplier, ALK, inhibitors

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