PR-924 |
Katalog-Nr.GC61945
One-Click Copy Product Info
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PR-924 ist ein selektiver LMP-7-Inhibitor der Tripeptid-Epoxyketon-Immunoproteasom-Untereinheit mit einem IC50-Wert von 22 nM. PR-924 modifiziert kovalent proteasomale N-terminale Threonin-Aktivstellen. PR-924 hemmt das Wachstum und lÖst die Apoptose in Zellen des multiplen Myeloms (MM) aus. PR-924 hat AntitumoraktivitÄten.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1416709-79-9
Sample solution is provided at 25 µL, 10mM.
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PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities[1][2].
PR-924 (1-20 µM; 24-72 hours; MM.1S, MM.1R, RPMI-8226, KMS12, LR-5, DOX40, INA-6, OPM1 and OPM2 cells) treatment significantly decreases the viability of all the MM cell lines in a time-and dose-dependent manner (IC 50 range for cell lines: 3-7 µM for 48 h)[1]. PR-924 (3 µM; 48 hours; MM.1S and MM.1R cells) treatment triggers apoptosis in MM cells[1]. PR-924 (3 µM; 48 hours; MM.1S and MM.1R cells) treatment triggers activation of caspase-3, caspase-8 and caspase-9, and significantly down-regulated the expression of Bcl-2 protein, without altering Bax or MCL-1 protein levels[1]. PR-924 induces BID cleavage and its translocation to mitochondria, as well as cyto-c release BID, a proapoptotic BH-3 family protein, is linked to mitochondria-mediated apoptotic signaling pathways via cyto-c release[1].
PR-924 (6 mg/kg; intravenous injection; twice a week; for 21 days; CB-17 SCID-mice) treatment significantly inhibits tumour growth in human plasmacytoma xenografts[1]. PR-924 treatment significant reduces the shIL-6R levels in SCID-hu model. Treatment of tumour-bearing mice with PR-924, prolongs survival[1].
References:
[1]. Singh AV, et al. PR-924, a selective inhibitor of the immunoproteasome subunit LMP-7, blocks multiple myeloma cell growth both in vitro and in vivo. Br J Haematol. 2011 Jan;152(2):155-63.
[2]. Parlati F, et al. Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome. Blood. 2009 Oct 15;114(16):3439-47.
| Cas No. | 1416709-79-9 | SDF | |
| Canonical SMILES | O=C(N[C@@H](CC1=CC=CC=C1)C([C@]2(CO2)C)=O)[C@@H](NC([C@@H](C)NC(C(CC3=CC=CC=C43)=C4C)=O)=O)CC5=CNC6=CC=CC=C56 | ||
| Formula | C37H38N4O5 | M.Wt | 618.72 |
| Löslichkeit | Storage | Store at -20°C | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6162 mL | 8.0812 mL | 16.1624 mL |
| 5 mM | 323.2 μL | 1.6162 mL | 3.2325 mL |
| 10 mM | 161.6 μL | 808.1 μL | 1.6162 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)