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RepSox

Catalog No. T6337 CAS 446859-33-2

Synonyms: ALK5 Inhibitor II, SJN 2511, E-616452

RepSox (ALK5 Inhibitor II) is a TGFβR-1/ALK5 inhibitor that selectively inhibits the binding of ATP to ALK5 and the autophosphorylation of ALK5 (IC50=23/4 nM). RepSox induces adipogenesis in MEFs cells.

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RepSox, CAS 446859-33-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 38.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 77.00
50 mg	In stock	Inquiry
1 mL * 10 mM (in DMSO)	In stock	$ 66.00

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Purity: 98.8%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	RepSox (ALK5 Inhibitor II) is a TGFβR-1/ALK5 inhibitor that selectively inhibits the binding of ATP to ALK5 and the autophosphorylation of ALK5 (IC50=23/4 nM). RepSox induces adipogenesis in MEFs cells.
Targets&IC50	TGFβRI:4 nM
In vitro	METHODS: Mouse embryonic fibroblast MEFs were treated with RepSox (10 µM) for 10 days and cellular lipids were detected using oil red O staining. RESULTS: Many adipocyte-like cells appeared in RepSox-treated MEFs, and oil red O staining of lipid droplets confirmed adipocyte differentiation. [1] METHODS: Sheep fibroblasts were treated with RepSox (10-25 nM) for 3 days, and cell morphology was observed using a microscope. RESULTS: After three days of RepSox treatment, sheep fibroblasts acquired a significantly different morphology and changed from a spindle shape to an elongated shape with more clusters. [2]
In vivo	METHODS: To test the effect on the differentiation of EGCs from intestinal glial cells, RepSox (3-10 mg/kg in 0.5% CMC-Na) was administered to GFAP-Cre:Rosa26-tdTomato mice by gavage once daily for two weeks. RESULTS: RepSox promotes the conversion of EGCs into neurons and improves gastrointestinal motility in vivo. [3] METHODS: To detect anti-tumor activity in vivo, RepSox (5-20 mg/kg) was injected intraperitoneally into a nude mouse model bearing osteosarcoma 143B every two days for three weeks. RESULTS: RepSox effectively inhibited the growth of osteosarcoma and had low toxicity in nude mice. [4]
Kinase Assay	The kinase domain of ALK5 is cloned by PCR and expressed in a baculovirus/Sf9 cells system. The protein is 6-His tagged in the C terminus and purified by affinity chromatography using a Ni2+column, and the obtained material is used to assess compound activity in an autophosphorylation assay. Purified enzyme (10 nM) is incubated in 50 μL of Tris buffer (Tris 50 mM, pH 7.4; NaCl, 100 mM; MgCl2, 5 mM; MnCl2, 5 mM; and DTT, 10 mM). The enzyme is preincubated with different concentrations of RepSox (0.1% DMSO final concentration in the test) for 10 min at 37°C. The reaction is then initiated by the addition of 3 μM ATP (0.5 μCi γ-33P-ATP). After 15 min at 37°C, phosphorylation is stopped by the addition of SDS?PAGE sample buffer (50 mM Tris-HCl, pH 6.9, 2.5% glycerol, 1% SDS, and 5% β-mercaptoethanol). The samples are boiled for 5 min at 95°C and run on a 12% SDS?PAGE. Dried gels are exposed to a phosphor screen overnight. ALK5 autophosphorylation is quantified using a Storm imaging system[1].
Cell Research	RepSox is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 1%) before use[1]. To test anti-TGF-β activity of compounds, HepG2 cells are seeded in 96 well microplates at a concentration of 35000 cells per well in 200 μL of serum-containing medium. The microplates are then placed for 24 h in a cell incubator at 37°C, 5% CO2 atm. RepSox dissolved in DMSO are then added at concentrations of 50 nM to 10 μM (final concentration of DMSO 1%) for 30 min prior to the addition of recombinant TGF-β (1 ng/mL). After an overnight incubation, the cells are washed with PBS and lysed by addition of 10 μL of passive lysis buffer. Inhibition of luciferase activity relative to control groups is used as a measure of compound activity. A concentration?response curve is constructed from which an IC50 value is determined graphically[1].

Synonyms	ALK5 Inhibitor II, SJN 2511, E-616452
Molecular Weight	287.32
Formula	C17H13N5
CAS No.	446859-33-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 53 mg/mL (184.5 mM)

References and Literature

1. Tu WZ, et al. RepSox, a small molecule inhibitor of the TGFβ receptor, induces brown adipogenesis and browning of white adipocytes. Acta Pharmacol Sin. 2019 Dec;40(12):1523-1531. 2. Guo Y, et al. RepSox effectively promotes the induced differentiation of sheep fibroblasts into adipocytes via the inhibition of the TGF‑β1/Smad pathway. Int J Mol Med. 2021 Aug;48(2):148. 3. Shi CJ, et al. TGFβR-1/ALK5 inhibitor RepSox induces enteric glia-to-neuron transition and influences gastrointestinal mobility in adult mice. Acta Pharmacol Sin. 2023 Jan;44(1):92-104. 4. He D, et al. TGF‑β inhibitor RepSox suppresses osteosarcoma via the JNK/Smad3 signaling pathway. Int J Oncol. 2021 Nov;59(5):84.

Citations

1. Ma X, Lu Y, Zhou Z, Human expandable pancreatic progenitor–derived β cells ameliorate diabetes. Science Advances. 2022, 8(8): eabk1826. 2. Wang W, Ren S, Lu Y, et al. Inhibition of Syk promotes chemical reprogramming of fibroblasts via metabolic rewiring and H2S production. The EMBO Journal. 2021 Jun 1;40(11):e106771. doi: 10.15252/embj.2020106771. Epub 2021 Apr 28. 3. Li J, Bai Y, Liu Y, et al.Transcriptome-based chemical screens identify CDK8 as a common barrier in multiple cell reprogramming systems.Cell Reports.2023, 42(6). 4. Zhang S, Lou H, Lu H, et al.Characterization of Proliferation Medium and Its Effect on Differentiation of Muscle Satellite Cells from Larimichthys crocea in Cultured Fish Meat Production.Fishes.2023, 8(9): 429.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library TGF-beta/Smad Compound Library Tyrosine Kinase Inhibitor Library Immuno-Oncology Compound Library Cytokine Inhibitor Library Bioactive Compound Library Human Metabolite Library Anti-Fibrosis Compound Library Anti-Colorectal Cancer Compound Library

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Keywords

RepSox 446859-33-2 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad TGF-β Receptor E 616452 E616452 ALK5 Inhibitor II SJN2511 Transforming growth factor beta receptors SJN-2511 SJN 2511 E-616452 Inhibitor inhibit inhibitor

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