SKL-2001 is a novel agonist of Wnt/β-catenin signaling pathway. SKL2001 suppresses colon cancer spheroid growth through regulation of the E-cadherin/β-Catenin complex. SKL2001 inhibited proliferation of colon cancer cells cultured in 3D spheroid and induced them accumulation in the G0/G1 phase of the cell cycle with a reduced c-myc level.
Chemical Formula: C14H14N4O3
Exact Mass: 286.1066
Molecular Weight: 286.291
Elemental Analysis: C, 58.74; H, 4.93; N, 19.57; O, 16.77
Wnt Agonist II;
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
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
SKL2001 is an agonist of the Wnt/β-catenin pathway, and also upregulates the expression of Axin2, a downstream target of the Wnt/β-catenin pathway, but shows no effect on NF-κB, p53 reporter activity and GSK-3β activity. SKL2001 causes osteoblast differentiation (20 and 40 μM) and suppresses preadipocyte differentiation (5, 10, and 30 μM) via the activation of the Wnt/β-catenin pathway. SKL2001 (5, 10, and 30 μM) stabilizes intracellular β-catenin in 3T3-L1 cells. SKL2001 (40 μM) significantly inhibits the proliferation of HCT116 spheroids independently of cytotoxicity and the inhibition is reversible; SKL2001 cuases cell cycle arrest in HCT116 spheroids. SKL2001 (40 μM) enhances round-shape spheroid formation and E-cadherin expression.
Jie Z, Shen S, Zhao X, Xu W, Zhang X, Huang B, Tang P, Qin A, Fan S, Xie Z. Activating β-catenin/Pax6 axis negatively regulates osteoclastogenesis by selectively inhibiting phosphorylation of p38/MAPK. FASEB J. 2018 Dec 7:fj201801977R. doi: 10.1096/fj.201801977R. [Epub ahead of print] PubMed PMID: 30526042.
Huang HL, Tang GD, Liang ZH, Qin MB, Wang XM, Chang RJ, Qin HP. Role of Wnt/β-catenin pathway agonist SKL2001 in Caerulein-induced acute pancreatitis. Can J Physiol Pharmacol. 2018 Oct 16:1-8. doi: 10.1139/cjpp-2018-0226. [Epub ahead of print] PubMed PMID: 30326193.
Guo C, Wang X, Chen LP, Li M, Li M, Hu YH, Ding WH, Wang X. Long non-coding RNA MALAT1 regulates ovarian cancer cell proliferation, migration and apoptosis through Wnt/β-catenin signaling pathway. Eur Rev Med Pharmacol Sci. 2018 Jun;22(12):3703-3712. doi: 10.26355/eurrev_201806_15249. PubMed PMID: 29949143.
Ohashi W, Yamamine N, Imura J, Hattori Y. SKL2001 suppresses colon cancer spheroid growth through regulation of the E-cadherin/β-Catenin complex. Biochem Biophys Res Commun. 2017 Nov 25;493(3):1342-1348. doi: 10.1016/j.bbrc.2017.09.161. Epub 2017 Sep 29. PubMed PMID: 28970068.
Li G, Liu J, Wang Y, Yang K, Zhao M, Xiao Y, Wen X, Liu L. LNGFR targets the Wnt/β-catenin pathway and promotes the osteogenic differentiation in rat ectomesenchymal stem cells. Sci Rep. 2017 Sep 8;7(1):11021. doi: 10.1038/s41598-017-11555-9. PubMed PMID: 28887537; PubMed Central PMCID: PMC5591262.
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