BYK204165


Catalog No. Size PriceQuantity
M20291-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1.

Product information

CAS Number: 1104546-89-5

Molecular Weight: 252.27

Formula: C15H12N2O2

Chemical Name: 4-[(1-methyl-1H-pyrrol-2-yl)methylidene]-1,2,3,4-tetrahydroisoquinoline-1,3-dione

Smiles: CN1C=CC=C1C=C1C2=CC=CC=C2C(=O)NC1=O

InChiKey: BTYSIDSTHDDAJW-LCYFTJDESA-N

InChi: InChI=1S/C15H12N2O2/c1-17-8-4-5-10(17)9-13-11-6-2-3-7-12(11)14(18)16-15(13)19/h2-9H,1H3,(H,16,18,19)/b13-9-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 125 mg/mL (495.50 mM; Need ultrasonic).

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:

In kinetic experiments with human PARP-1, BYK204165 exhibits potent and competitive inhibition of enzyme activity, yielding a pKi value of 7.05. BYK204165 exhibits low potency of PARP inhibition in C4I cells (pIC50 of 5.75).

In Vivo:

BYK204165 is not investigated in vivo because of its short half-time (t1/2) of 23 min measured at rat microsomes in vitro.

Products are for research use only. Not for human use.

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