ISA-2011B is an inhibitor of phosphatidylinositol-4-phosphate 5-kinase-α (PIP5Kα). ISA-2011B has anti-proliferative activity and induces apoptosis of prostate cancer cells.

 

Brand: BCM

 

In Vitro: ISA-2011B leads to a remarkable reduction in AR-V7 and CDK1 in both nucleus and cytoplasm of 22Rv1 cells. ISA-2011B shows the highest binding affinity to PIP5K1α, and to MAP/microtubule affinity-regulating kinase 1 and 4 (MARK1 and MARK4) across 460 kinases. ISA-2011B treatment inhibits PIP5K1α expression by 78.6% in PC-3 cells. ISA-2011B treatment also abolishes AR expression in the nucleus, without depleting the cytoplasmic AR. The proliferation rate of PC-3 cells after treatment with ISA-2011B at 10, 20, and 50 μM is obviously reduced to 58.77%, 48.65%, and 21.62% of vehicle-treated controls, respectively.

 

Boiling Point: 714.9±60.0 °C(Predicted)

 

pKa: 15.58±0.30(Predicted)

 

Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water.

 

Isomeric SMILES: CN1CC(=O)N2[C@H](C1=O)CC3=CC4=C(C=C3[C@H]2C5=CNC6=C5C=C(C=C6)Cl)OCO4  

 

InChIKey: FSEZESVJDPKRDS-UWJYYQICSA-N  

 

InChI: InChI=1S/C22H18ClN3O4/c1-25-9-20(27)26-17(22(25)28)4-11-5-18-19(30-10-29-18)7-13(11)21(26)15-8-24-16-3-2-12(23)6-14(15)16/h2-3,5-8,17,21,24H,4,9-10H2,1H3/t17-,21-/m0/s1

 

Attribute
[Chem Name]	(2S,8S)-2-(5-chloro-1H-indol-3-yl)-6-methyl-13,15-dioxa-3,6-diazatetracyclo[8.7.0.03,8.012,16]heptadeca-1(17),10,12(16)-triene-4,7-dione
[Synonym]	ISA-2011B
[CAS No.]	1395347-24-6
[MDL No.]	MFCD30533398
[Formula]	C22H18ClN3O4
[Molecular]	423.85
[Form]	Solid Powder
[Storage]	Sealed in dry. Store in freezer, under -20°C

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