Free shipping on all orders over $ 500

RepSox (ALK5 Inhibitor II)

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

RepSox; E-616452; SJN 2511; 616452

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 50  USD50 In stock
10mg USD 75  USD75 In stock
25mg USD 150  USD150 In stock
50mg USD 265  USD265 In stock
100mg USD 435  USD435 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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
Method
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.
Protocol (for reference only)
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
Dosages
Administration
Chemical Information
Molecular Weight 287.32
Formula C17H13N5
CAS Number 446859-33-2
Solubility (25°C) DMSO ≥ 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Luo ZB, et al. Reprod Fertil Dev. Cotreatment with RepSox and LBH589 improves the invitro developmental competence of porcine somatic cell nuclear transfer embryos.

[2] Ide M, et al. Exp Dermatol. Transforming growth factor β-inhibitor Repsox downregulates collagen expression of scleroderma dermal fibroblasts and prevents bleomycin-induced mice skin fibrosis.

[3] Zhu HY, et al. Biotechnol Lett. RepSox improves viability and regulates gene expression in rhesus monkey-pig interspecies cloned embryos.

[4] Ichida JK, et al. Cell Stem Cell. A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog.

[5] Gellibert F, et al. J Med Chem. Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.

Related ALK Products
NVL-655

NVL-655 is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 has an IC50 of 2.7 nM. It can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC).

APG-2449

APG-2449 is an orally active, potent ALK/ROS1/FAK inhibitor with anti-tumor activity in a mouse model of non-small cell lung cancer (NSCLC).

ALK2-IN-5

ALK2-IN-5, pyrazolopyrimidine compound, is an ALK2 inhibitor.

J-1048

J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor.

CPD-1224

CPD-1224 is an orally active derivative of ALK inhibitors to cereblon ligands.

  Catalog
Abmole Inhibitor Catalog




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


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.