RepSox | ALK5 Inhibitor II | SJN-2511 | E 616452 | CAS#446859-33-2 | ALK5 Inhibitor

MedKoo Cat#: 406816 | Name: RepSox

Description:

WARNING: This product is for research use only, not for human or veterinary use.

RepSox, also known as SJN 2511, E 616452 and ALK5 inhibitor II, is a cell permeable, selective inhibitor of the TGF-β type 1 activin like kinase receptor ALK5

Chemical Structure

RepSox

CAS#446859-33-2

Theoretical Analysis

MedKoo Cat#: 406816

Name: RepSox

CAS#: 446859-33-2

Chemical Formula: C17H13N5

Exact Mass: 287.1171

Molecular Weight: 287.33

Elemental Analysis: C, 71.06; H, 4.56; N, 24.37

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 2,650.00	2 Weeks
1g	USD 3,650.00	2 Weeks
2g	USD 6,450.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

E 616452; E-616452; E616452; RepSox; SJN 2511; SJN-2511; SJN-2511; ALK5 Inhibitor II

IUPAC/Chemical Name

2-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]-1,5-naphthyridine

InChi Key

LBPKYPYHDKKRFS-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)

SMILES Code

CC1=CC=CC(C2=NNC=C2C3=NC4=CC=CN=C4C=C3)=N1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO and ethanol

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO and ethanol

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

RepSox acts as a potent, selective, reversible, and ATP-competitive inhibitor of TGF-β type I receptor (ALK5; IC50 = 23 nM, 4 nM and 18 nM for ALK5 binding, ALK5 auto-phosphorylation and TGF-β cellular assay in HepG2 cells, respectively). It minimally affects a panel of 9 closely related kinases, including p38 MAPK at IC50 >16 µM.

In vitro activity:

Protein levels of molecules associated with the epithelial‑mesenchymal transition phenotype, including E‑cadherin, N‑cadherin, Vimentin, matrix metalloproteinase (MMP)‑2 and MMP‑9, were reduced by RepSox treatment. Reference: Int J Oncol. 2021 Nov;59(5):84. https://pubmed.ncbi.nlm.nih.gov/34533199/

In vivo activity:

RepSox-induced neurons were Calbindin- and nNOS-positive and displayed typical neuronal electrophysiological properties. The administration of RepSox (3, 10 mg· kg-1 ·d-1, i.g.) for 2 weeks significantly promoted the conversion of enteric glial cells to neurons in the enteric nervous system and influenced gastrointestinal motility in adult mice. Reference: Acta Pharmacol Sin. 2023 Jan;44(1):92-104. https://pubmed.ncbi.nlm.nih.gov/35794374/

	Solvent	mg/mL	mM
Solubility
	DMSO	28.7	100.00
	Ethanol	5.8	20.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 287.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. He D, Gao J, Zheng L, Liu S, Ye L, Lai H, Pan B, Pan W, Lou C, Chen Z, Fan S. TGF‑β inhibitor RepSox suppresses osteosarcoma via the JNK/Smad3 signaling pathway. Int J Oncol. 2021 Nov;59(5):84. doi: 10.3892/ijo.2021.5264. Epub 2021 Sep 17. PMID: 34533199; PMCID: PMC8460063. 2. Jajosky AN, Coad JE, Vos JA, Martin KH, Senft JR, Wenger SL, Gibson LF. RepSox slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression. Stem Cells Transl Med. 2014 Jul;3(7):836-48. doi: 10.5966/sctm.2013-0193. Epub 2014 May 22. PMID: 24855276; PMCID: PMC4073822. 3. Shi CJ, Lian JJ, Zhang BW, Cha JX, Hua QH, Pi XP, Hou YJ, Xie X, Zhang R. 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. doi: 10.1038/s41401-022-00932-4. Epub 2022 Jul 6. PMID: 35794374; PMCID: PMC9813375. 4. Guo Y, Zhu H, Li X, Ma C, Li Y, Sun T, Wang Y, Wang C, Guan W, Liu C. 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. doi: 10.3892/ijmm.2021.4981. Epub 2021 Jun 16. PMID: 34132357; PMCID: PMC8208630.

In vitro protocol:

In vivo protocol:

1. Shi CJ, Lian JJ, Zhang BW, Cha JX, Hua QH, Pi XP, Hou YJ, Xie X, Zhang R. 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. doi: 10.1038/s41401-022-00932-4. Epub 2022 Jul 6. PMID: 35794374; PMCID: PMC9813375. 2. Guo Y, Zhu H, Li X, Ma C, Li Y, Sun T, Wang Y, Wang C, Guan W, Liu C. 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. doi: 10.3892/ijmm.2021.4981. Epub 2021 Jun 16. PMID: 34132357; PMCID: PMC8208630.

1: Xu D, Liu G, Zhao M, Wan X, Qu Y, Murayama R, Hashimoto K. Effects of arketamine on depression-like behaviors and demyelination in mice exposed to chronic restrain stress: A role of transforming growth factor-β1. J Affect Disord. 2024 Sep 3;367:745-755. doi: 10.1016/j.jad.2024.08.222. Epub ahead of print. PMID: 39236893. 2: Liu W, Long L, Wang Z, He S, Han Y, Yang L, Hu C, Wang Y. A Whole-Course- Repair System Based on Stimulus-Responsive Multifunctional Hydrogels for Myocardial Tissue Regeneration. Small Methods. 2024 Jun 25:e2400121. doi: 10.1002/smtd.202400121. Epub ahead of print. PMID: 38923800. 3: Sharifi-Kelishadi M, Zare L, Fathollahi Y, Javan M. Conversion of Astrocyte Cell Lines to Oligodendrocyte Progenitor Cells Using Small Molecules and Transplantation to Animal Model of Multiple Sclerosis. J Mol Neurosci. 2024 Apr 9;74(2):40. doi: 10.1007/s12031-024-02206-6. PMID: 38594388. 4: Wang W, Yang T, Chen S, Liang L, Wang Y, Ding Y, Xiong W, Ye X, Guo Y, Shen S, Chen H, Chen J. Tissue engineering RPE sheet derived from hiPSC-RPE cell spheroids supplemented with Y-27632 and RepSox. J Biol Eng. 2024 Jan 16;18(1):7. doi: 10.1186/s13036-024-00405-8. PMID: 38229139; PMCID: PMC10790375. 5: Guo D, Zhang B, Han L, Rensing NR, Wong M. Cerebral vascular and blood brain- barrier abnormalities in a mouse model of epilepsy and tuberous sclerosis complex. Epilepsia. 2024 Feb;65(2):483-496. doi: 10.1111/epi.17848. Epub 2023 Dec 16. PMID: 38049961; PMCID: PMC10922951. 6: Taga H, Kishida T, Inoue Y, Yamamoto K, Kotani SI, Masashi T, Ukimura O, Mazda O. TGF-β inhibitor treatment of H₂O₂-induced cystitis models provides biochemical mechanism for elucidating interstitial cystitis/painful bladder syndrome patients. PLoS One. 2023 Nov 6;18(11):e0293983. doi: 10.1371/journal.pone.0293983. PMID: 37931000; PMCID: PMC10627456. 7: Lietuvninkas L, Baccouche B, Kazlauskas A. The Multi-Kinase Inhibitor RepSox Enforces Barrier Function in the Face of Both VEGF and Cytokines. Biomedicines. 2023 Aug 31;11(9):2431. doi: 10.3390/biomedicines11092431. PMID: 37760872; PMCID: PMC10525881. 8: Pitt K, Mochida Y, Senoo M. Greener Grass: The Modern History of Epithelial Stem Cell Innovation. Life (Basel). 2023 Mar 3;13(3):688. doi: 10.3390/life13030688. PMID: 36983843; PMCID: PMC10058258. 9: Sun L, Zhang D, Qin L, Liu Q, Wang G, Shi D, Huang B. Rapid direct conversion of bovine non-adipogenic fibroblasts into adipocyte-like cells by a small- molecule cocktail. Front Cell Dev Biol. 2023 Feb 2;11:1020965. doi: 10.3389/fcell.2023.1020965. PMID: 36819108; PMCID: PMC9932023. 10: Liu L, Jouve C, Henry J, Berrandou TE, Hulot JS, Georges A, Bouatia-Naji N. Genomic, Transcriptomic, and Proteomic Depiction of Induced Pluripotent Stem Cells-Derived Smooth Muscle Cells As Emerging Cellular Models for Arterial Diseases. Hypertension. 2023 Apr;80(4):740-753. doi: 10.1161/HYPERTENSIONAHA.122.19733. Epub 2023 Jan 19. PMID: 36655574. 11: Xu J, Fang S, Deng S, Li H, Lin X, Huang Y, Chung S, Shu Y, Shao Z. Generation of neural organoids for spinal-cord regeneration via the direct reprogramming of human astrocytes. Nat Biomed Eng. 2023 Mar;7(3):253-269. doi: 10.1038/s41551-022-00963-6. Epub 2022 Nov 24. PMID: 36424465. 12: Xu J, Li Y, Zhu H, Wu W, Liu Y, Guo Y, Guan W, Liu C, Ma C. Therapeutic function of a novel rat induced pluripotent stem cell line in a 6‑OHDA‑induced rat model of Parkinson's disease. Int J Mol Med. 2022 Dec;50(6):140. doi: 10.3892/ijmm.2022.5196. Epub 2022 Oct 27. PMID: 36300203; PMCID: PMC9652010. 13: Guo Y, Wang YY, Sun TT, Xu JJ, Yang P, Ma CY, Guan WJ, Wang CJ, Liu GF, Liu CQ. Neural progenitor cells derived from fibroblasts induced by small molecule compounds under hypoxia for treatment of Parkinson's disease in rats. Neural Regen Res. 2023 May;18(5):1090-1098. doi: 10.4103/1673-5374.355820. PMID: 36254998; PMCID: PMC9827776. 14: Wang YY, Sun TT, Yang P, Xu JJ, Liang Y, Wu F, Ma CY, Wang CJ, Liu CQ, Guo Y. [VCR, a Small Molecule Compound, Induces Reprogramming of Rat Fibroblasts into Neural Progenitor Cells under Hypoxic Condition]. Sichuan Da Xue Xue Bao Yi Xue Ban. 2022 Sep;53(5):790-797. Chinese. doi: 10.12182/20220960501. PMID: 36224680; PMCID: PMC10408786. 15: Lee K, Ahn HS, Estevez B, Poncz M. RUNX1-deficient human megakaryocytes demonstrate thrombopoietic and platelet half-life and functional defects. Blood. 2023 Jan 19;141(3):260-270. doi: 10.1182/blood.2022017561. PMID: 36219879; PMCID: PMC9936297. 16: Yoon JY, Mandakhbayar N, Hyun J, Yoon DS, Patel KD, Kang K, Shim HS, Lee HH, Lee JH, Leong KW, Kim HW. Chemically-induced osteogenic cells for bone tissue engineering and disease modeling. Biomaterials. 2022 Oct;289:121792. doi: 10.1016/j.biomaterials.2022.121792. Epub 2022 Sep 8. Erratum in: Biomaterials. 2022 Nov;290:121822. doi: 10.1016/j.biomaterials.2022.121822. PMID: 36116170. 17: Shi CJ, Lian JJ, Zhang BW, Cha JX, Hua QH, Pi XP, Hou YJ, Xie X, Zhang R. 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. doi: 10.1038/s41401-022-00932-4. Epub 2022 Jul 6. PMID: 35794374; PMCID: PMC9813375. 18: Wang X, Wu J, Wang W, Zhang Y, He D, Xiao B, Zhang H, Song A, Xing Y, Li B. Reprogramming of Rat Fibroblasts into Induced Neurons by Small-Molecule Compounds In Vitro and In Vivo. ACS Chem Neurosci. 2022 Jul 20;13(14):2099-2109. doi: 10.1021/acschemneuro.2c00078. Epub 2022 Jun 20. PMID: 35723446. 19: Fernandes GS, Singh RD, Kim KK. Generation of a Pure Culture of Neuron-like Cells with a Glutamatergic Phenotype from Mouse Astrocytes. Biomedicines. 2022 Apr 18;10(4):928. doi: 10.3390/biomedicines10040928. PMID: 35453678; PMCID: PMC9031297. 20: Kim BK, Canonica J, Roudnicky F, Westenskow PD. Preventing VEGF-Mediated Vascular Permeability by Experimentally Potentiating BBB Characteristics in Endothelial Cells. Methods Mol Biol. 2022;2475:259-274. doi: 10.1007/978-1-0716-2217-9_19. PMID: 35451764.