Biological Activity

Bortezomib (PS-341) is a highly selective, reversible inhibitor of the 26S proteasome with a ki value of 6nM, which has shown high antimyeloma activity. Bortezomib caused comparable growth suppression in LNCaP-Pro5 and PC3M-Pro4 cells with an IC90 of 10 nM.

Product Citations

• 

  Cancer Lett. 2024 Apr 6;590:216861.

  TRAF6 enhances PD-L1 expression through YAP1-TFCP2 signaling in melanoma
  Bortezomib (PS-341) purchased from AbMole

• 

  Mol Ther Oncol. 2024 Apr 11;32(2):200802.

  Bortezomib promotes the TRAIL-mediated killing of resistant rhabdomyosarcoma by ErbB2/Her2-targeted CAR-NK-92 cells via DR5 upregulation
  Bortezomib (PS-341) purchased from AbMole

• 

  Cell Death Differ. 2023 Mar 9.

  Targeting HDAC3 to overcome the resistance to ATRA or arsenic in acute promyelocytic leukemia through ubiquitination and degradation of PML-RARα
  Bortezomib (PS-341) purchased from AbMole

• 

  BMC Biol. 2023 Apr 7;21(1):75.

  1, 6-Hexanediol regulates angiogenesis via suppression of cyclin A1-mediated endothelial function
  Bortezomib (PS-341) purchased from AbMole

• 

  Sci Rep. 2020 Feb 25;10(1):3386.

  Gender-specific Changes in Energy Metabolism and Protein Degradation as Major Pathways Affected in Livers of Mice Treated With Ibuprofen
  Bortezomib (PS-341) purchased from AbMole

• 

  Cell Physiol Biochem. 2018;50(6):2341-2364.

  Peperomin E Induces Promoter Hypomethylation of Metastatic-Suppressor Genes and Attenuates Metastasis in Poorly Differentiated Gastric Cancer.
  Bortezomib (PS-341) purchased from AbMole

• 

  Int J Oncol. 2016 Oct;49(4):1469-78.

  Metabotropic glutamate receptor 3 is involved in B-cell-related tumor apoptosis
  Bortezomib (PS-341) purchased from AbMole

Customer Product Validations & Biological Datas

	Source	INTERNATIONAL JOURNAL OF ONCOLOGY (2016) . Figure 9. Bortezomib (M1686) was from Abmole Bioscience Inc. (Houston, TX, USA)
	Method	FACS
	Cell Lines	B cells from CD19 cre/+Foxo1F/+ and CD19 cre/+Foxo1F/F mice
	Concentrations	0.05 μg/ml
	Incubation Time	24 h
	Results	The effect of Foxo1-defciency on cell apoptosis was approved by using B cells from CD19cre/+Foxo1F/+ and CD19cre/+Foxo1F/F (Fig. 9D).

	Source	INTERNATIONAL JOURNAL OF ONCOLOGY (2016) . Figure 5. MBortezomib (M1686) was from Abmole Bioscience Inc. (Houston, TX, USA)
	Method	FACS
	Cell Lines	SP2/0 cells
	Concentrations	0, 0.05 and 0.25 μg/ml
	Incubation Time	24 h
	Results	Low dose of bortezomib, frst-line drug in patients with newly diagnosed multiple myeloma, could effectively induce apoptosis and Grm3 expression (Fig. 5).

Protocol (for reference only)

Cell Experiment
Cell lines	Nine canine melanoma cell lines (CMM-1, CMM-2, ChMC, KMeC, LMeC, OMJ, OMS, OMK, and NML)
Preparation method	Cell growth inhibition assay Nine canine melanoma cell lines (CMM-1, CMM-2, ChMC, KMeC, LMeC, OMJ, OMS, OMK, and NML) were cultured in 96-well plates (2 *102 cells/well) for 24 h in cDMEM and treated with different concentrations of bortezomib (0–100 nM) for 72 h. Cell viability was then measured by a WST-1 cell proliferation assay kit (Takara) and the half maximal inhibitory concentration (IC50) of bortezomib for each cell line was calculated using the GraphPad Prism software (GraphPad Software).
Concentrations	0–100 nM
Incubation time	72 h

Animal Experiment
Animal models	CMM-1 cells in xenograft mouse models
Formulation	100 µL PBS containing 4.2% DMSO
Dosages	0.8mg/kg twice weekly
Administration	intravenous(IV) injections

Chemical Information

Molecular Weight	384.24
Formula	C19H25BN4O4
CAS Number	179324-69-7
Solubility (25°C)	DMSO 72 mg/mL
Storage	2-8°C, protect from light

References

[1] Andrew Sandstrom, et al. Science. Functional degradation: A mechanism of NLRP1 inflammasome activation by diverse pathogen enzymes

[2] Ashley J Chui, et al. Science. N-terminal degradation activates the NLRP1B inflammasome

[3] Koda et al. Rinsho Ketsueki. Early onset of paralytic ileus caused by simultaneous administration of bortezomib and azole antifungals in multiple myeloma patients.

[4] Rushworth et al. Cell Signal. BTK inhibitor ibrutinib is cytotoxic to myeloma and potently enhances bortezomib and lenalidomide activities through NF-κB.

[5] Chauhan et al. Cancer Cell. A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance.

[6] Jung et al. Am J Hematol. Synergistic anticancer effects of arsenic trioxide with bortezomib in mantle cell lymphoma.