BMS-P5
BMS-P5 Basic information
- Product Name:
- BMS-P5
- Synonyms:
-
- NET,BMS P5,myeloma,inhibit,Peptidylarginine Deiminase,Inhibitor,Protein Arginine Deiminase,Multiple,BMS-P5,BMS-P-5,BMSP5
- ((2S,5S)-5-amino-2-methylpiperidin-1-yl)(2-(1-(cyclopropylmethyl)-1H-pyrrolo[2,3-b]pyridin-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone hydrochloride
- BMS-P5 HCL
- BMS-P5, 10 mM in DMSO
- [(2S,5R)-5-amino-2-methylpiperidin-1-yl]-[2-[1-(cyclopropylmethyl)pyrrolo[2,3-b]pyridin-2-yl]-7-methoxy-1-methylbenzimidazol-5-yl]methanone
- CAS:
- 1549811-36-0
- MF:
- C27H33ClN6O2
- MW:
- 509.05
- Mol File:
- 1549811-36-0.mol
BMS-P5 Chemical Properties
- form
- Solid
- color
- Off-white to light yellow
- InChIKey
- UMXWDEKCDIDCBA-TVJVWYQLNA-N
- SMILES
- C(C1CC1)N1C2=NC=CC=C2C=C1C1=NC2=CC(C(N3C[C@H](N)CC[C@@H]3C)=O)=CC(OC)=C2N1C.Cl |&1:21,25,r|
BMS-P5 Usage And Synthesis
Description
BMS-P5 is a Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor with pIC50 values in the range of 5-7.5. BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma. Administration of BMS-P5 to multiple myeloma-bearing mice delays appearance of symptoms and disease progression Targeting PAD4 may be beneficial for treatment of multiple myeloma.
Uses
BMS-P5 is a selective and orally active peptidylarginine deiminase 4 (PAD4) inhibitor with an IC50 of 98 nM. BMS-P5 shows selective for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 blocks multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and delays progression of MM in a syngeneic mouse model[1].
Biological Activity
BMS-P5 is an inhibitor of the protein arginine deiminase 4 (PAD4; IC50 = 0.098 μM). It is selective for PAD4 over PAD1, -2, and -3 (IC50s = >10 μM). BMS-P5 (1 μM) inhibits citrullination of histone H3 and neutrophil extracellular trap (NET) formation induced by RPMI-8226- or MM.1S-conditioned medium in isolated human neutrophils. It delays disease onset and increases survival in a DP42 syngeneic mouse model of multiple myeloma when administered at a dose of 50 mg/kg.
in vivo
BMS-P5 (50 mg/kg, oral gavage) significantly improves survival of MM-bearing mice[1].
BMS-P5 (50 mg/kg, oral gavage) may attenuate the presence of pro-tumorigenic proteins in the tumor microenvironment, and thus delay tumor progression[1].
| Animal Model: | Syngeneic mouse model of MM[1]. |
| Dosage: | 50 mg/kg. |
| Administration: | Oral gavage, twice a day beginning on day 3 after tumor cell injection. |
| Result: | Significantly delayed development of symptoms and significantly prolonged survival of MM-bearing mice. |
References
[1] Marina Li, et al. A Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma. Mol Cancer Ther. 2020 Jul;19(7):1530-1538. DOI:10.1158/1535-7163.MCT-19-1020
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