Bortezomib free base · Synonyms: Brotezamide | LDP 341 | MG 341

Bortezomib is a reversible and selective proteasome inhibitor.

For research use only. Not for human or veterinary use.

Target Proteasome NF-κB Apoptosis Autophagy TREM receptor Ligands for Target Protein for PROTAC

Research area Cancer

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Data Sheet SDS COA

Bortezomib structure

CAS No.: 179324-69-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
10 g	USD 565.00	BP-01928-10g	In stock	Get quote
25 g	USD 965.00	BP-01928-25g	In stock	Get quote

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Description

Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.

Biological activity

In Vitro Bortezomib (PS-341) (100 nM; 8 hours) results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1. Bortezomib (PS-341) (5-100 nM; 20 hours) induces apoptosis in mantle-cell lymphoma (MCL) cell lines. Bortezomib (PS-341) (20 nM; 1-14 hours) induces Noxa up-regulation in both MCL cell lines. The IC50 of Bortezomib (PS-341) is found to be 2.46 nM for 26S proteasome in the B16F10 cells. Bortezomib (PS-341) suppresses several anti-apoptotic proteins (e.g., Bcl-XL, Bcl-2, and STAT-3). In Vivo Bortezomib (PS-341) (0.3-1 mg/kg; i.v.; once weekly for 4 weeks) inhibits PC-3 Tumor Growth in Nude Mice.

Identifiers

SMILES: CC(C)C[C@@H](B(O)O)NC([C@@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2)=O
InChIKey: GXJABQQUPOEUTA-RDJZCZTQSA-N

Specifications

MW (average): 384.2370
Formula: C₁₉H₂₅BN₄O₄
CAS No.: 179324-69-7
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: 4°C, protect from light

Solubility

Soluble in Ethanol : 66.67 mg/mL DMSO : 50 mg/mL

Documents

References

[1]. Adams J, et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer Res. 1999 Jun 1;59(11):2615-22.

[2]. Shahshahan MA, et al. Potential usage of proteasome inhibitor bortezomib (Velcade, PS-341) in the treatment of metastaticmelanoma: basic and clinical aspects. Am J Cancer Res. 2011;1(7):913-24.

[3]. Pérez-Galán P, et al. The proteasome inhibitor bortezomib induces apoptosis in mantle-cell lymphoma through generation of ROS and Noxa activation independent of p53 status. Blood. 2006 Jan 1;107(1):257-64.

[4]. Yerlikaya A, et al. Combined effects of the proteasome inhibitor bortezomib and Hsp70 inhibitors on the B16F10 melanoma cell line. Mol Med Rep. 2010 Mar-Apr;3(2):333-9.

[5]. Mujtaba T, et al. Advances in the understanding of mechanisms and therapeutic use of bortezomib. Discov Med. 2011 Dec;12(67):471-80.

[6]. Fernández Y, et al. Chemical blockage of the proteasome inhibitory function of bortezomib: impact on tumor cell death. J Biol Chem. 2006 Jan 13;281(2):1107-18.

[7]. Wang Y, et al. TREM2-Mediated Cholesterol Efflux in Macrophages Inhibits Anti-Tumor Immunity via Limitation of CD4+ T and NK Cells. Adv Sci (Weinh). 2025 Oct 20:e06995.

Same target

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Same research area

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