Grouped product items

SKU

Size

Availability

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A288659-10mg

10mg

In stock

$142.90

A288659-50mg

50mg

In stock

$454.90

A288659-250mg

250mg

Available within 4-8 weeks(?)

$2,047.90

Basic Description

Synonyms	A-366\|1527503-11-2\|A 366\|5'-methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3'-indol]-2'-amine\|A366\|5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine\|CHEMBL3109630\|5'-methoxy-6'-(3-pyrrolidin-1-ylpropoxy)spiro[
Specifications & Purity	Moligand™, ≥98%(HPLC)
Biochemical and Physiological Mechanisms	Potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50= 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. Decreases levels of lysine 9 dimethylation on histone H3 (H3K9Me2) in PC3 cells.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of euchromatic histone lysine methyltransferase 1;Inhibitor of euchromatic histone lysine methyltransferase 2

Associated Targets

DNMT1 Tclin DNA (cytosine-5)-methyltransferase 1 0 Activities

Discover Target: DNMT1

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

EHMT2 Tchem Histone-lysine N-methyltransferase EHMT2 7 Activities

Discover Target: EHMT2

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

DOT1L Tchem Histone-lysine N-methyltransferase, H3 lysine-79 specific 0 Activities

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

EZH1 Tchem Histone-lysine N-methyltransferase EZH1 0 Activities

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

EZH2 Tclin Histone-lysine N-methyltransferase EZH2 0 Activities

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

EHMT1 Tchem Histone-lysine N-methyltransferase EHMT1 3 Activities

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

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

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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)

EED Tchem Polycomb protein EED 0 Activities

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

SUV39H2 Tchem Histone-lysine N-methyltransferase SUV39H2 0 Activities

Discover Target: SUV39H2

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

SPIN1 Tchem Spindlin-1 6 Activities

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

SPIN3 Tchem Spindlin-3 0 Activities

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

SPIN4 Tchem Spindlin-4 0 Activities

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

KMT2A Tchem Histone-lysine N-methyltransferase 2A 0 Activities

Discover Target: KMT2A

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

KMT5A Tchem N-lysine methyltransferase KMT5A 0 Activities

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

KMT5B Tchem Histone-lysine N-methyltransferase KMT5B 0 Activities

Discover Target: KMT5B

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

HDAC6 Tclin Histone deacetylase 6 0 Activities

Discover Target: HDAC6

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

KMT5C Tchem Histone-lysine N-methyltransferase KMT5C 0 Activities

Discover Target: KMT5C

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)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

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

SPIN2B Tchem Spindlin-2B 0 Activities

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

SETDB1 Tbio Histone-lysine N-methyltransferase SETDB1 0 Activities

Discover Target: SETDB1

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

SMYD3 Tchem Histone-lysine N-methyltransferase SMYD3 0 Activities

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

SMYD2 Tchem N-lysine methyltransferase SMYD2 0 Activities

Discover Target: SMYD2

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

SETD2 Tchem Histone-lysine N-methyltransferase SETD2 0 Activities

Discover Target: SETD2

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

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Discover Target: TRIM24

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

SETD7 Tchem Histone-lysine N-methyltransferase SETD7 0 Activities

Discover Target: SETD7

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

RBBP5 Tbio Retinoblastoma-binding protein 5 0 Activities

Discover Target: RBBP5

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

PRMT5 Tchem Protein arginine N-methyltransferase 5 0 Activities

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

BRPF1 Tchem Peregrin 0 Activities

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

PRMT1 Tchem Protein arginine N-methyltransferase 1 0 Activities

Discover Target: PRMT1

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)

PRMT8 Tchem Protein arginine N-methyltransferase 8 0 Activities

Discover Target: PRMT8

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)

PRMT6 Tchem Protein arginine N-methyltransferase 6 0 Activities

Discover Target: PRMT6

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

PRMT3 Tchem Protein arginine N-methyltransferase 3 0 Activities

Discover Target: PRMT3

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)

NSD2 Tchem Histone-lysine N-methyltransferase NSD2 0 Activities

Discover Target: NSD2

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

NSD3 Tchem Histone-lysine N-methyltransferase NSD3 0 Activities

Discover Target: NSD3

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

WDR77 Tbio Methylosome protein 50 0 Activities

Discover Target: WDR77

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

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Discover Target: MAPK1

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

Names and Identifiers

IUPAC Name	5'-methoxy-6'-(3-pyrrolidin-1-ylpropoxy)spiro[cyclobutane-1,3'-indole]-2'-amine
INCHI	InChI=1S/C19H27N3O2/c1-23-16-12-14-15(21-18(20)19(14)6-4-7-19)13-17(16)24-11-5-10-22-8-2-3-9-22/h12-13H,2-11H2,1H3,(H2,20,21)
InChi Key	BKCDJTRMYWSXMC-UHFFFAOYSA-N
Canonical SMILES	COC1=C(C=C2C(=C1)C3(CCC3)C(=N2)N)OCCCN4CCCC4
Isomeric SMILES	COC1=C(C=C2C(=C1)C3(CCC3)C(=N2)N)OCCCN4CCCC4
WGK Germany	3
Alternate CAS	1527503-11-2
PubChem CID	76285486
MeSH Entry Terms	5'-methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro(cyclobutane-1,3'-indol)-2'-amine;A-366 compound
Molecular Weight	329.44

Certificates

Certificate of Analysis(COA)

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3 results found

Lot Number	Certificate Type	Date	Item
J2112131	Certificate of Analysis	Jul 19, 2024	A288659
J2112132	Certificate of Analysis	Jul 19, 2024	A288659
J2112133	Certificate of Analysis	Jul 19, 2024	A288659

Chemical and Physical Properties

Solubility	Solvent:1eq. HCl, Max Conc. mg/mL: 32.94, Max Conc. mM: 100; Solvent:DMSO, Max Conc. mg/mL: 32.94, Max Conc. mM: 100

Safety and Hazards(GHS)

Pictogram(s)	GHS09
Signal	Warning
Hazard Statements	H400:Very toxic to aquatic life H410:Very toxic to aquatic life with long lasting effects
Precautionary Statements	P273:Avoid release to the environment. P501:Dispose of contents/container to ... P391:Collect spillage.
WGK Germany	3
RIDADR	UN30779/PGIII

References

1. Sweis RF, Pliushchev M, Brown PJ, Guo J, Li F, Maag D, Petros AM, Soni NB, Tse C, Vedadi M et al.. (2014) Discovery and development of potent and selective inhibitors of histone methyltransferase g9a.. ACS Med Chem Lett, 5 (2): (205-9). [PMID:24900801]

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A 366 - ≥98%(HPLC), high purity , CAS No.1527503-11-2, Inhibitor of euchromatic histone lysine methyltransferase 1;Inhibitor of euchromatic histone lysine methyltransferase 2