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lorecivivint , CAS No.L611570, Inhibitor of CDC like kinase 2;Inhibitor of dual specificity tyrosine phosphorylation regulated kinase 1A

  • Moligand™
Item Number
L611570
Grouped product items
SKUSizeAvailabilityPrice Qty
L611570-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,334.90
L611570-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,001.90

Basic Description

SynonymsAdavivint|lorecivivint|1467093-03-3|SM04690|N-(5-(3-(7-(3-Fluorophenyl)-3H-imidazo[4,5-c]pyridin-2-yl)-1H-indazol-5-yl)pyridin-3-yl)-3-methylbutanamide|Lorecivivint [USAN]|SM-04690|Adavivint (SM04690)|42EK42WHI5|1467093-03-3 (free base)|N-(5-(3-(7-(3-Fluo
Specifications & PurityMoligand™
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of CDC like kinase 2;Inhibitor of dual specificity tyrosine phosphorylation regulated kinase 1A

Associated Targets

DYRK1B Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DYRK2 Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DYRK3 Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DYRK4 Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DYRK1A Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK5R1 Tchem Cyclin-dependent kinase 5 activator 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSNK1E Tclin Casein kinase I isoform epsilon 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK1 Tchem Dual specificity protein kinase CLK1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK2 Tchem Dual specificity protein kinase CLK2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK4 Tchem Dual specificity protein kinase CLK4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name N-(5-{3-[7-(3-fluorophenyl)-1H-imidazo[4,5-c]pyridin-2-yl]-1H-indazol-5-yl}pyridin-3-yl)-3-methylbutanamide
INCHI InChI=1S/C29H24FN7O/c1-16(2)8-26(38)33-21-10-19(12-31-13-21)17-6-7-24-22(11-17)28(37-36-24)29-34-25-15-32-14-23(27(25)35-29)18-4-3-5-20(30)9-18/h3-7,9-16H,8H2,1-2H3,(H,33,38)(H,34,35)(H,36,37)
InChi Key AQDWDWAYVBQMAM-UHFFFAOYSA-N
Canonical SMILES CC(CC(=O)Nc1cncc(c1)c1ccc2c(c1)c(n[nH]2)c1nc2c([nH]1)c(cnc2)c1cccc(c1)F)C
Isomeric SMILES CC(C)CC(=O)NC1=CN=CC(=C1)C2=CC3=C(C=C2)NN=C3C4=NC5=C(N4)C=NC=C5C6=CC(=CC=C6)F
PubChem CID 135565709

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References

1. Yates KE, Shortkroff S, Reish RG.  (2005)  Wnt influence on chondrocyte differentiation and cartilage function..  DNA Cell Biol,  24  (7): (446-57).  [PMID:16008513]
2. Blom AB, Brockbank SM, van Lent PL, van Beuningen HM, Geurts J, Takahashi N, van der Kraan PM, van de Loo FA, Schreurs BW, Clements K et al..  (2009)  Involvement of the Wnt signaling pathway in experimental and human osteoarthritis: prominent role of Wnt-induced signaling protein 1..  Arthritis Rheum,  60  (2): (501-12).  [PMID:19180479]
3. Maeda A, Ono M, Holmbeck K, Li L, Kilts TM, Kram V, Noonan ML, Yoshioka Y, McNerny EM, Tantillo MA et al..  (2015)  WNT1-induced Secreted Protein-1 (WISP1), a Novel Regulator of Bone Turnover and Wnt Signaling..  J Biol Chem,  290  (22): (14004-18).  [PMID:25864198]
4. Yazici Y, McAlindon TE, Fleischmann R, Gibofsky A, Lane NE, Kivitz AJ, Skrepnik N, Armas E, Swearingen CJ, DiFrancesco A et al..  (2017)  A novel Wnt pathway inhibitor, SM04690, for the treatment of moderate to severe osteoarthritis of the knee: results of a 24-week, randomized, controlled, phase 1 study..  Osteoarthr Cartil,  25  (10): (1598-1606).  [PMID:28711582]
5. Deshmukh V, Hu H, Barroga C, Bossard C, Kc S, Dellamary L, Stewart J, Chiu K, Ibanez M, Pedraza M et al..  (2018)  A small-molecule inhibitor of the Wnt pathway (SM04690) as a potential disease modifying agent for the treatment of osteoarthritis of the knee..  Osteoarthr Cartil,  26  (1): (18-27).  [PMID:28888902]
6. Deshmukh V, O'Green AL, Bossard C, Seo T, Lamangan L, Ibanez M, Ghias A, Lai C, Do L, Cho S et al..  (2019)  Modulation of the Wnt pathway through inhibition of CLK2 and DYRK1A by lorecivivint as a novel, potentially disease-modifying approach for knee osteoarthritis treatment..  Osteoarthr Cartil,  27  (9): (1347-1360).  [PMID:31132406]

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