PKCθ;inhibitor 14 , CAS No.P612855, Inhibitor of protein kinase C theta

Item Number
P612855
Grouped product items
SKUSizeAvailabilityPrice Qty
P612855-5mg
5mg
In stock
$572.90
P612855-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,000.90

Basic Description

SynonymsPKCtheta inhibitor 14 | PKCtheta inhibitor 14 | CHEMBL3798011 | GTPL9452 | BDBM50166588 | compound 14 [PMID: 27117263]
Specifications & PurityMoligand™, ≥98%
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of protein kinase C theta
Product Description

PKCθ inhibitor 14 was developed using structure-based drug design . The compound is described as being selective for PKCθ, over other kinases, including related PKC isoforms.

Associated Targets(Human)

PRKCQ Tchem Protein kinase C theta type (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
INSR Tclin Insulin receptor (5558 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PRKCZ Tchem Protein kinase C zeta (2414 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ROCK1 Tclin Rho-associated protein kinase 1 (4723 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PLK1 Tchem Serine/threonine-protein kinase PLK1 (28605 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
JAK1 Tclin Tyrosine-protein kinase JAK1 (8569 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPKAPK2 Tchem MAP kinase-activated protein kinase 2 (4814 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ROCK2 Tclin Rho-associated protein kinase 2 (6206 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTK2 Tclin Focal adhesion kinase 1 (4730 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 (4127 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MET Tclin Hepatocyte growth factor receptor (10718 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PRKCA Tchem Protein kinase C alpha (5923 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPK3 Tchem MAP kinase ERK1 (4725 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NTRK1 Tclin Nerve growth factor receptor Trk-A (7922 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PRKCQ Tchem Protein kinase C theta (3319 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHEK1 Tchem Serine/threonine-protein kinase Chk1 (6846 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
IRAK4 Tchem Interleukin-1 receptor-associated kinase 4 (5917 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CLK1 Tchem Dual specificty protein kinase CLK1 (2189 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EPHA5 Tchem Ephrin type-A receptor 5 (1056 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP3K5 Tchem Mitogen-activated protein kinase kinase kinase 5 (1965 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDC7 Tchem Cell division cycle 7-related protein kinase (1385 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

PIK3CA PI3-kinase p110-alpha subunit (51 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Prkcd Protein kinase C delta (192 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Prkcb Protein kinase C beta (2 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Plasma (328 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Whole blood (71 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 2,2-dimethyl-7-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)-1-[(1R)-1-phenylethyl]-3H-quinazolin-4-one
INCHI InChI=1S/C24H23N5O2/c1-15(16-8-5-4-6-9-16)29-20-14-17(11-12-18(20)22(30)27-24(29,2)3)28-19-10-7-13-25-21(19)26-23(28)31/h4-15H,1-3H3,(H,27,30)(H,25,26,31)/t15-/m1/s1
InChi Key WNYKGJHEQVIFGL-OAHLLOKOSA-N
Canonical SMILES O=C1NC(C)(C)N(c2c1ccc(c2)n1c(=O)[nH]c2c1cccn2)[C@@H](c1ccccc1)C
Isomeric SMILES C[C@H](C1=CC=CC=C1)N2C3=C(C=CC(=C3)N4C5=C(NC4=O)N=CC=C5)C(=O)NC2(C)C
PubChem CID 91933875
Molecular Weight 413.5

Certificates

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4 results found

Lot NumberCertificate TypeDateItem
H2420006Certificate of AnalysisAug 15, 2024 P612855
H2420007Certificate of AnalysisAug 15, 2024 P612855
H2420009Certificate of AnalysisAug 15, 2024 P612855
H2420010Certificate of AnalysisAug 15, 2024 P612855

Related Documents

References

1. Katoh T, Takai T, Yukawa T, Tsukamoto T, Watanabe E, Mototani H, Arita T, Hayashi H, Nakagawa H, Klein MG et al..  (2016)  Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKCθ inhibitors..  Bioorg Med Chem,  24  (11): (2466-75).  [PMID:27117263] [10.1021/op500134e]

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