WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 401002
Description: A-83-01 is an ALK inhibibitor. It was found that A-83-01 inhibited the transcriptional activity induced by TGF-beta type I receptor ALK-5 and that by activin type IB receptor ALK-4 and nodal type I receptor ALK-7, the kinase domains of which are structurally highly related to those of ALK-5. A-83-01 was found to be more potent in the inhibition of ALK5 than a previously described ALK-5 inhibitor, SB-431542, and also to prevent phosphorylation of Smad2/3 and the growth inhibition induced by TGF-beta. A-83-01 inhibited the epithelial-to-mesenchymal transition induced by TGF-beta, suggesting that A-83-01 and related molecules may be useful for preventing the progression of advanced cancers.
MedKoo Cat#: 401002
Chemical Formula: C25H19N5S
Exact Mass: 421.13612
Molecular Weight: 421.52
Elemental Analysis: C, 71.23; H, 4.54; N, 16.61; S, 7.61
Synonym: A8301; A 8301; A-8301
IUPAC/Chemical Name: 3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide
InChi Key: HIJMSZGHKQPPJS-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H19N5S/c1-17-8-7-13-23(27-17)24-21(19-14-15-26-22-12-6-5-11-20(19)22)16-30(29-24)25(31)28-18-9-3-2-4-10-18/h2-16H,1H3,(H,28,31)
SMILES Code: S=C(N1N=C(C2=NC(C)=CC=C2)C(C3=CC=NC4=CC=CC=C34)=C1)NC5=CC=CC=C5
Appearance: white 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, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
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
The following data is based on the product molecular weight 421.52 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|
1: Spinato S, Galindo-Moreno P, Zaffe D, Bernardello F, Soardi CM. Is socket healing conditioned by buccal plate thickness? A clinical and histologic study 4 months after mineralized human bone allografting. Clin Oral Implants Res. 2012 Nov 21. doi: 10.1111/clr.12073. [Epub ahead of print] PubMed PMID: 23167308.
2: Chen WP, Wu SM. Small molecule regulators of postnatal Nkx2.5 cardiomyoblast proliferation and differentiation. J Cell Mol Med. 2012 May;16(5):961-5. doi: 10.1111/j.1582-4934.2011.01513.x. PubMed PMID: 22212626; PubMed Central PMCID: PMC3325363.
3: Shimada H, Hashimoto Y, Nakada A, Shigeno K, Nakamura T. Accelerated generation of human induced pluripotent stem cells with retroviral transduction and chemical inhibitors under physiological hypoxia. Biochem Biophys Res Commun. 2012 Jan 13;417(2):659-64. doi: 10.1016/j.bbrc.2011.11.111. Epub 2011 Dec 8. PubMed PMID: 22172948.
4: Vogt J, Traynor R, Sapkota GP. The specificities of small molecule inhibitors of the TGFÃŸ and BMP pathways. Cell Signal. 2011 Nov;23(11):1831-42. doi: 10.1016/j.cellsig.2011.06.019. Epub 2011 Jun 29. PubMed PMID: 21740966.
5: Yamamura S, Matsumura N, Mandai M, Huang Z, Oura T, Baba T, Hamanishi J, Yamaguchi K, Kang HS, Okamoto T, Abiko K, Mori S, Murphy SK, Konishi I. The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. Int J Cancer. 2012 Jan 1;130(1):20-8. doi: 10.1002/ijc.25961. Epub 2011 Apr 18. PubMed PMID: 21503873.
6: Yuan X, Wan H, Zhao X, Zhu S, Zhou Q, Ding S. Brief report: combined chemical treatment enables Oct4-induced reprogramming from mouse embryonic fibroblasts. Stem Cells. 2011 Mar;29(3):549-53. doi: 10.1002/stem.594. PubMed PMID: 21425417.
7: Yu J, Chau KF, Vodyanik MA, Jiang J, Jiang Y. Efficient feeder-free episomal reprogramming with small molecules. PLoS One. 2011 Mar 1;6(3):e17557. doi: 10.1371/journal.pone.0017557. PubMed PMID: 21390254; PubMed Central PMCID: PMC3046978.
8: Furutani Y, Umemoto T, Murakami M, Matsui T, Funaba M. Role of endogenous TGF-β family in myogenic differentiation of C2C12 cells. J Cell Biochem. 2011 Feb;112(2):614-24. doi: 10.1002/jcb.22953. PubMed PMID: 21268083.
9: Yuan X, Wan H, Zhao X, Zhu S, Zhou Q, Ding S. Combined Chemical Treatment Enables Oct4-Induced Reprogramming from Mouse Embryonic Fibroblasts. Stem Cells. 2011 Jan 7. [Epub ahead of print] PubMed PMID: 21218442.
10: Kawano K, Maitani Y. [Tumor permeability of nanocarriers observed by dynamic contrast-enhanced magnetic resonance imaging]. Yakugaku Zasshi. 2010 Dec;130(12):1679-85. Review. Japanese. PubMed PMID: 21139395.
11: Taniguchi Y, Kawano K, Minowa T, Sugino T, Shimojo Y, Maitani Y. Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13. doi: 10.1111/j.1349-7006.2010.01646.x. Epub 2010 Jul 1. PubMed PMID: 20608940.
12: Minowa T, Kawano K, Kuribayashi H, Shiraishi K, Sugino T, Hattori Y, Yokoyama M, Maitani Y. Increase in tumour permeability following TGF-beta type I receptor-inhibitor treatment observed by dynamic contrast-enhanced MRI. Br J Cancer. 2009 Dec 1;101(11):1884-90. doi: 10.1038/sj.bjc.6605367. Epub 2009 Nov 3. PubMed PMID: 19888220; PubMed Central PMCID: PMC2788254.
13: Hoberg M, Rudert M, Pap T, Klein G, Gay S, Aicher WK. Attachment to laminin-111 facilitates transforming growth factor beta-induced expression of matrix metalloproteinase-3 in synovial fibroblasts. Ann Rheum Dis. 2007 Apr;66(4):446-51. Epub 2006 Nov 23. PubMed PMID: 17124250; PubMed Central PMCID: PMC1856036.
14: Tojo M, Hamashima Y, Hanyu A, Kajimoto T, Saitoh M, Miyazono K, Node M, Imamura T. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005 Nov;96(11):791-800. PubMed PMID: 16271073.