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.
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
 . figure 9..jpg) |
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). |
 . figure 5..jpg) |
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). |
| 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 |
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Ashley J Chui, et al. Science. N-terminal degradation activates the NLRP1B inflammasome
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| Acetyl-Calpastatin(184-210)(human) TFA
Acetyl-Calpastatin(184-210)(human) TFA is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively. |
| Dazcapistat
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| Rpn11-IN-1
Rpn11-IN-1 (Capzimin intermediate) is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM. |
| (Rac)-Calpain Inhibitor XII
(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM). (Rac)-Calpain Inhibitor XII has lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). |
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