Product Name :
PR-924
Description:
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.
CAS:
1416709-79-9
Molecular Weight:
618.72
Formula:
C37H38N4O5
Chemical Name:
(2S)-3-(1H-indol-3-yl)-2-[(2R)-2-[(3-methyl-1H-inden-2-yl)formamido]propanamido]-N-[(2S)-1-[(2R)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]propanamide
Smiles :
CC1C2=CC=CC=C2CC=1C(=O)N[C@H](C)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)[C@@]1(C)CO1
InChiKey:
ADBUEVSHEJICCM-LZNHGOJSSA-N
InChi :
InChI=1S/C37H38N4O5/c1-22-27-14-8-7-13-25(27)18-29(22)35(44)39-23(2)34(43)41-32(19-26-20-38-30-16-10-9-15-28(26)30)36(45)40-31(33(42)37(3)21-46-37)17-24-11-5-4-6-12-24/h4-16,20,23,31-32,38H,17-19,21H2,1-3H3,(H,39,44)(H,40,45)(H,41,43)/t23-,31+,32+,37-/m1/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Nusinersen} MedChemExpress|{Nusinersen} DNA/RNA Synthesis|{Nusinersen} Protocol|{Nusinersen} In stock|{Nusinersen} supplier|{Nusinersen} Epigenetic Reader Domain}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.|Product information|CAS Number: 1416709-79-9|Molecular Weight: 618.72|Formula: C37H38N4O5|Chemical Name: (2S)-3-(1H-indol-3-yl)-2-[(2R)-2-[(3-methyl-1H-inden-2-yl)formamido]propanamido]-N-[(2S)-1-[(2R)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]propanamide|Smiles: CC1C2=CC=CC=C2CC=1C(=O)N[C@H](C)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)[C@@]1(C)CO1|InChiKey: ADBUEVSHEJICCM-LZNHGOJSSA-N|InChi: InChI=1S/C37H38N4O5/c1-22-27-14-8-7-13-25(27)18-29(22)35(44)39-23(2)34(43)41-32(19-26-20-38-30-16-10-9-15-28(26)30)36(45)40-31(33(42)37(3)21-46-37)17-24-11-5-4-6-12-24/h4-16,20,23,31-32,38H,17-19,21H2,1-3H3,(H,39,44)(H,40,45)(H,41,43)/t23-,31+,32+,37-/m1/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|PR-924 (1-20 μM; 24-72 hours; MM.{{Romosozumab} MedChemExpress|{Romosozumab} Purity & Documentation|{Romosozumab} In Vitro|{Romosozumab} manufacturer|{Romosozumab} Epigenetic Reader Domain} 1S, MM.PMID:23554582 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). PR-924 (3 μM; 48 hours; MM.1S and MM.1R cells) treatment triggers apoptosis in MM cells. 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. 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.|In Vivo:|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. PR-924 treatment significant reduces the shIL-6R levels in SCID-hu model. Treatment of tumour-bearing mice with PR-924, prolongs survival.|References:|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.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.Products are for research use only. Not for human use.|