| Identification | Back Directory | [Name]
5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine | [CAS]
1527503-11-2 | [Synonyms]
A-366
A-336
CS-2077
A-366; A366;A 366
5'-methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3'-indol]-2'-amine
5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine
Spiro[cyclobutane-1,3'-[3H]indol]-2'-amine, 5'-methoxy-6'-[3-(1-pyrrolidinyl)propoxy]- | [EINECS(EC#)]
808-907-0 | [Molecular Formula]
C19H27N3O2 | [MDL Number]
MFCD28133403 | [MOL File]
1527503-11-2.mol | [Molecular Weight]
329.44 |
| Chemical Properties | Back Directory | [Boiling point ]
533.6±60.0 °C(Predicted) | [density ]
1.29±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO : 50 mg/mL (151.77 mM; Need ultrasonic) | [form ]
powder | [pka]
10.18±0.20(Predicted) | [color ]
white to beige | [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) | [InChIKey]
BKCDJTRMYWSXMC-UHFFFAOYSA-N | [SMILES]
C12(C3=C(N=C1N)C=C(OCCCN1CCCC1)C(OC)=C3)CCC2 |
| Hazard Information | Back Directory | [Uses]
A-366 acts as a potent peptide-competitive inhibitor of the lysine methyltransferase G9a. 1000 fold selectivity over other methyl transferases. | [Biochem/physiol Actions]
A-366 is an SGC chemical probe for G9a/GLP, developed in collaboration with Abbvie. A-366 is a potent, selective inhibitor of the histone methyltransferase G9a. The IC50 values for G9a inhbition in enzymatic and cell based assays are 3.3 and approximately 3 μM, respectively. A-366 has little or no detectable activity against a panel of 21 other methyltransferases. For full characterization details, please visit the A-366 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc | [in vivo]
A-366 (30 mg/kg; osmotic mini-pump; daily for 14 days) treatment of MV4;11 xenografts elicits growth inhibition[4]. | Animal Model: | 6-8 week old SCID-beige female mice (MV4;11 xenografts)[4] | | Dosage: | 30 mg/kg | | Administration: | By osmotic mini-pump; daily for 14 days | | Result: | A modest 45% tumor growth inhibition resulting from A-366 treatment in this model.
|
| [IC 50]
EHMT2/G9a/KMT1C; EHMT1/GLP/KMT1D | [storage]
Store at -20°C |
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| Company Name: |
DKMbiochem.Co. Ltd Gold
|
| Tel: |
15901859516 |
| Website: |
http://www.dkmbiochem.com/ |
| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
|