Bortezomib is a potent protease inhibitor with a Ki of 0.6 nM. It showed good selectivity to tumor cells. Bortezomib inhibits NF-κB and induces phosphorylation of ERK to inhibit cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.

 

Brand: BCM

 

Target: Apoptosis; NF-κB; Proteasome; Autophagy

Signaling Pathways: Apoptosis; Autophagy; NF-κB; Proteases/Proteasome; Ubiquitination

 

In Vitro: The average growth inhibition of 50% (GI50) value for Bortezomib across the entire NCI cell panel was 7 nM. Bortezomib was shown to penetrate into cells and inhibit proteasome-mediated intracellular proteolysis of long-lived proteins (IC50: ～0.1 μM). Exposure to bortezomib has been shown to stabilize p21, p27, and p53, as well as the proapoptotic Bid and Bax proteins, caveolin-1. Bortezomib also promoted the activation of the proapoptotic c-Jun-NH2 terminal kinase, as well as the endoplasmic reticulum stress response. Bortezomib (0.01-10 μM) treatment caused cell accumulation at the G2-M phase and induced cell apoptotic death in a concentration-dependent manner. The slower mobility of the Bcl-2 band corresponded to the phosphorylation of the Bcl-2 protein and could be seen in the cells exposed to 0.01–0.05 μM Bortezomib for 24 h. Another slower band could be discerned, which corresponded to a superphosphorylated form of Bcl-2, and was detected when cells were exposed to higher concentrations of Bortezomib (0.1–10 μM) for 24 h.

 

Melting Point: 122-124°C

 

pKa: 9.66±0.43(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethnaol.

 

GHS: GHS06, GHS08

 

Isomeric SMILES: B([C@H](CC(C)C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O  

 

InChIKey: GXJABQQUPOEUTA-RDJZCZTQSA-N  

 

InChI: InChI=1S/C19H25BN4O4/c1-13(2)10-17(20(27)28)24-18(25)15(11-14-6-4-3-5-7-14)23-19(26)16-12-21-8-9-22-16/h3-9,12-13,15,17,27-28H,10-11H2,1-2H3,(H,23,26)(H,24,25)/t15-,17-/m0/s1

 

Attribute
[Chem Name]	[(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid
[Synonym]	Bortezomib; LDP-341; MLM341; NSC 681239; PS-341
[CAS No.]	179324-69-7
[EINECS]	605-854-3
[MDL No.]	MFCD09056737
[Formula]	C19H25BN4O4
[Molecular]	384.24
[Form]	White solid
[Storage]	Keep in dark place. Inert atmosphere, 2-8°C

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