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

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

MedKoo CAT#: 406816

CAS#: 446859-33-2

Description: 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

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406816
Name: RepSox
CAS#: 446859-33-2
Chemical Formula: C17H13N5
Exact Mass: 287.12
Molecular Weight: 287.330
Elemental Analysis: C, 71.06; H, 4.56; N, 24.37

Price and Availability

Size	Price	Availability
50mg	USD 450	2 Weeks
100mg	USD 750	2 Weeks
200mg	USD 1250	2 Weeks
500mg	USD 2650	2 Weeks
1g	USD 3650	2 Weeks
2g	USD 6450	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

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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/

Solubility Data

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

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:	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.
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.

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1: Fu Y, Huang C, Xu X, Gu H, Ye Y, Jiang C, Qiu Z, Xie X. Direct reprogramming of mouse fibroblasts into cardiomyocytes with chemical cocktails. Cell Res. 2015 Sep;25(9):1013-24. doi: 10.1038/cr.2015.99. Epub 2015 Aug 21. PubMed PMID: 26292833; PubMed Central PMCID: PMC4559819.

2: Lv L, Han Q, Chu Y, Zhang M, Sun L, Wei W, Jin C, Li W. Self-renewal of hepatoblasts under chemically defined conditions by iterative growth factor and chemical screening. Hepatology. 2015 Jan;61(1):337-47. doi: 10.1002/hep.27421. Epub 2014 Dec 15. PubMed PMID: 25203445.

3: 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. PubMed PMID: 24855276; PubMed Central PMCID: PMC4073822.

4: Wu MZ, Li M, Liu GH, Izpisua Belmonte JC. A chemical approach to "rewire" neural progenitor cells. Cell Res. 2014 Jun;24(6):641-2. doi: 10.1038/cr.2014.51. Epub 2014 Apr 18. PubMed PMID: 24743789; PubMed Central PMCID: PMC4042174.

5: Cheng L, Hu W, Qiu B, Zhao J, Yu Y, Guan W, Wang M, Yang W, Pei G. Generation of neural progenitor cells by chemical cocktails and hypoxia. Cell Res. 2014 Jun;24(6):665-79. doi: 10.1038/cr.2014.32. Epub 2014 Mar 18. Erratum in: Cell Res. 2015 May;25(5):645-6. PubMed PMID: 24638034; PubMed Central PMCID: PMC4042166.

6: Liu X, Sun H, Qi J, Wang L, He S, Liu J, Feng C, Chen C, Li W, Guo Y, Qin D, Pan G, Chen J, Pei D, Zheng H. Sequential introduction of reprogramming factors reveals a time-sensitive requirement for individual factors and a sequential EMT-MET mechanism for optimal reprogramming. Nat Cell Biol. 2013 Jul;15(7):829-38. doi: 10.1038/ncb2765. Epub 2013 May 26. PubMed PMID: 23708003.

7: Solanki A, Lee KB. A step closer to complete chemical reprogramming for generating iPS cells. Chembiochem. 2010 Apr 12;11(6):755-7. doi: 10.1002/cbic.201000032. PubMed PMID: 20183843; PubMed Central PMCID: PMC2967350.

8: Ichida JK, Blanchard J, Lam K, Son EY, Chung JE, Egli D, Loh KM, Carter AC, Di Giorgio FP, Koszka K, Huangfu D, Akutsu H, Liu DR, Rubin LL, Eggan K. A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog. Cell Stem Cell. 2009 Nov 6;5(5):491-503. doi: 10.1016/j.stem.2009.09.012. Epub 2009 Oct 8. PubMed PMID: 19818703; PubMed Central PMCID: PMC3335195.

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