1. Epigenetics
  2. Protein Arginine Deiminase
  3. BMS-P5

BMS-P5 

目录号: HY-137655
产品使用指南

BMS-P5 是特异性的、具有口服活性的肽精氨酸二亚胺酶 4 (PAD4) 的抑制剂。BMS-P5 可阻断多发性骨髓瘤诱导的 NET 形成,并延缓肿瘤进程。

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BMS-P5 Chemical Structure

BMS-P5 Chemical Structure

CAS No. : 1549811-36-0

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Description

BMS-P5 is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model[1].

In Vitro

BMS-P5 blocks calcium ionophore-induced citrullination of histone H3[1].
BMS-P5 is also able to inhibit formation of NETs induced by primary MM cells isolated from the BM of patients with MM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Neutrophils.
Concentration: 10 µM and 100 µM.
Incubation Time: 30 min followed by addition of DP42 or 5TGM1 CM.
Result: Prevented MM-induced NET formation.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

509.04

Formula

C₂₇H₃₃ClN₆O₂

CAS No.

1549811-36-0

SMILES

O=C(N1[C@@H](C)CC[C@@H](N)C1)C2=CC(OC)=C3C(N=C(C4=CC5=CC=CN=C5N4CC6CC6)N3C)=C2.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

BMS-P5Protein Arginine DeiminasePeptidylarginine DeiminaseMultiplemyelomaNETInhibitorinhibitorinhibit

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产品名称:
BMS-P5
目录号:
HY-137655
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