| Chemical Properties | Back Directory | [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| |
| Hazard Information | Back Directory | [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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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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