BMS-P5

Product Name: BMS-P5
CAS No.: 1549811-36-0
Chemical Name: BMS-P5
Synonyms: BMS-P5 HCL;BMS-P5, 10 mM in DMSO;NET,BMS P5,myeloma,inhibit,Peptidylarginine Deiminase,Inhibitor,Protein Arginine Deiminase,Multiple,BMS-P5,BMS-P-5,BMSP5;[(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;((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
CBNumber: CB29731093
Molecular Formula: C27H33ClN6O2
Formula Weight: 509.05
MOL File: 1549811-36-0.mol

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BMS-P5 Property

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|

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Hazard and Precautionary Statements (GHS)

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BMS-P5 Chemical Properties,Usage,Production

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

BMS-P5 Preparation Products And Raw materials

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View Lastest Price from BMS-P5 manufacturers

Hubei Chuchang Biotech Co., Ltd.

Product: BMS-P5 1549811-36-0
Price: US $0.00-0.00/MG
Min. Order: 1MG
Purity: 98
Supply Ability: 100G
Release date: 2024-04-17

1549811-36-0, BMS-P5Related Search:

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

1549811-36-0