Grouped product items

SKU

Size

Availability

Price

Qty

G610617-5mg

5mg

Available within 8-12 weeks(?)

$1,334.90

G610617-25mg

25mg

Available within 8-12 weeks(?)

$2,001.90

Basic Description

Synonyms	example 152 [WO2014111496]
Specifications & Purity	Moligand™
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of mitogen-activated protein kinase kinase kinase 12

Associated Targets

CHP1 Tbio Calcineurin B homologous protein 1 0 Activities

Discover Target: CHP1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK1 Tchem Cyclin-dependent kinase 1 0 Activities

Discover Target: CDK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD2 Tclin D(2) dopamine receptor 0 Activities

Discover Target: DRD2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ERBB4 Tclin Receptor tyrosine-protein kinase erbB-4 0 Activities

Discover Target: ERBB4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ERBB2 Tclin Receptor tyrosine-protein kinase erbB-2 0 Activities

Discover Target: ERBB2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 0 Activities

Discover Target: GABRA1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EGFR Tclin Epidermal growth factor receptor 0 Activities

Discover Target: EGFR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Discover Target: CDK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT4 Tclin Vascular endothelial growth factor receptor 3 0 Activities

Discover Target: FLT4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

YES1 Tclin Tyrosine-protein kinase Yes 0 Activities

Discover Target: YES1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 0 Activities

Discover Target: TYK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

Discover Target: FLT3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Discover Target: FGFR3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HRH1 Tclin Histamine H1 receptor 0 Activities

Discover Target: HRH1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MET Tclin Hepatocyte growth factor receptor 0 Activities

Discover Target: MET

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

IGF1R Tclin Insulin-like growth factor 1 receptor 0 Activities

Discover Target: IGF1R

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A4 Tclin Sodium-dependent serotonin transporter 0 Activities

Discover Target: SLC6A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIM1 Tchem Serine/threonine-protein kinase pim-1 0 Activities

Discover Target: PIM1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 0 Activities

Discover Target: PIK3CG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRA Tclin Platelet-derived growth factor receptor alpha 0 Activities

Discover Target: PDGFRA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RPS6KA2 Tchem Ribosomal protein S6 kinase alpha-2 0 Activities

Discover Target: RPS6KA2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKCH Tchem Protein kinase C eta type 0 Activities

Discover Target: PRKCH

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BTK Tclin Tyrosine-protein kinase BTK 0 Activities

Discover Target: BTK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Discover Target: AURKA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKB Tchem Aurora kinase B 0 Activities

Discover Target: AURKB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TNK2 Tclin Activated CDC42 kinase 1 0 Activities

Discover Target: TNK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM3 Tclin Muscarinic acetylcholine receptor M3 0 Activities

Discover Target: CHRM3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2B Tclin Alpha-2B adrenergic receptor 0 Activities

Discover Target: ADRA2B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A 0 Activities

Discover Target: HTR2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADORA2A Tclin Adenosine receptor A2a 0 Activities

Discover Target: ADORA2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ACHE Tclin Acetylcholinesterase 0 Activities

Discover Target: ACHE

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Discover Target: ABL1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT2 Tchem RAC-beta serine/threonine-protein kinase 0 Activities

Discover Target: AKT2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 0 Activities

Discover Target: AKT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADORA1 Tclin Adenosine receptor A1 0 Activities

Discover Target: ADORA1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR1A Tclin 5-hydroxytryptamine receptor 1A 0 Activities

Discover Target: HTR1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR3A Tclin 5-hydroxytryptamine receptor 3A 0 Activities

Discover Target: HTR3A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B 0 Activities

Discover Target: HTR2B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

Discover Target: CLK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EDNRA Tclin Endothelin-1 receptor 0 Activities

Discover Target: EDNRA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Discover Target: GSK3B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KIT Tclin Mast/stem cell growth factor receptor Kit 0 Activities

Discover Target: KIT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

OPRD1 Tclin Delta-type opioid receptor 0 Activities

Discover Target: OPRD1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NTRK1 Tclin High affinity nerve growth factor receptor 0 Activities

Discover Target: NTRK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TACR1 Tclin Substance-P receptor 0 Activities

Discover Target: TACR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MTOR Tclin Serine/threonine-protein kinase mTOR 0 Activities

Discover Target: MTOR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	5-[1-(cyclopropylmethyl)-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine
INCHI	InChI=1S/C21H24F3N5O/c22-21(23,24)16-3-12(5-26-20(16)25)17-4-18(29(27-17)6-11-1-2-11)19-14-7-28(8-15(14)19)13-9-30-10-13/h3-5,11,13-15,19H,1-2,6-10H2,(H2,25,26)/t14-,15+,19+
InChi Key	IRPVABHDSJVBNZ-QWHZDKJVSA-N
Canonical SMILES	Nc1ncc(cc1C(F)(F)F)c1nn(c(c1)[C@@H]1[C@@H]2[C@H]1CN(C2)C1COC1)CC1CC1
Isomeric SMILES	C1CC1CN2C(=CC(=N2)C3=CC(=C(N=C3)N)C(F)(F)F)C4[C@H]5[C@@H]4CN(C5)C6COC6
PubChem CID	90292687

Database links

PubChem CID	90292687
ChEMBL Ligand	CHEMBL3715238

Certificates

Certificate of Analysis(COA)

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References

1. Siu M, Sengupta Ghosh A, Lewcock JW. (2018) Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration.. J Med Chem, 61 (18): (8078-8087). [PMID:29863360]

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SKU	Size	Availability	Price	Qty
G610617-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,334.90
G610617-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$2,001.90

GNE-8505 , CAS No.G610617, Inhibitor of mitogen-activated protein kinase kinase kinase 12