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SM04690

Chemical Structure : SM04690

CAS No.: 1467093-03-3

SM04690 (Adavivint, Lorecivivint, SM-04690, SM 04690)

Catalog No.: PC-60504Not For Human Use, Lab Use Only.

Adavivint (Lorecivivint, SM04690) is a novel small molecule Wnt pathway inhibitor with EC50 of 3 nM in vitro, potently inhibits CLK2 and DYRK1A with IC50 of 5.8 and 26.9 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Adavivint (Lorecivivint, SM04690) is a novel small molecule Wnt pathway inhibitor with EC50 of 3 nM in vitro, potently inhibits CLK2 and DYRK1A with IC50 of 5.8 and 26.9 nM, respectively.
SM04690 demonstrates selectivity against a panel of 318 kinases, showes ≥90% inhibition of 7 kinases (out of 318) at 0.5 uM.
SM04690 inhibits CLK- and DYRK1A-mediated signaling in hMSCs and chondrocytes, 2–300-fold more potent than CC-671, TG003, ML167, Leucettine L41, ML315.
SM04690 dose dependently inhibited the CLK-mediated phosphorylation of SRSF4, SRSF5, and SRSF6 in hMSCs and human chondrocytes.
SM04690 induces hMSC differentiation into mature, functional chondrocytes and decreases cartilage catabolic marker levels.
SM04690 significantly improves Osteoarthritis Research Society International (OARSI) histology scores and biomarkers in a rodent OA model.

Physicochemical Properties

M.Wt 505.557
Formula C29H24FN7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(5-{3-[7-(3-fluorophenyl)-1H-imidazo[4,5-c]pyridin-2-yl]-1H-indazol-5-yl}pyridin-3-yl)-3-methylbutanamide

References

1. Yazici Y, et al. Osteoarthritis Cartilage. 2017 Jul 13. pii: S1063-4584(17)31085-3.
2. Deshmukh V, et al. Osteoarthritis Cartilage. 2017 Sep 6. pii: S1063-4584(17)31167-6.
3. V Deshmukh, et al. Osteoarthritis Cartilage. 2019 Sep;27(9):1347-1360. 

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