BQR-695


Catalog No. Size PriceQuantity
M14694-2 2mg solid $105
M14694-10 10mg solid $315

Description

BQR-695 is a PI4KIIIβ inhibitor with IC50s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.

Product information

CAS Number: 1513879-21-4

Molecular Weight: 352.39

Formula: C19H20N4O3

Chemical Name: 2-{[7-(3,4-dimethoxyphenyl)quinoxalin-2-yl]amino}-N-methylacetamide

Smiles: CNC(=O)CNC1=CN=C2C=CC(=CC2=N1)C1=CC(OC)=C(C=C1)OC

InChiKey: LYPCULYCGFOIDA-UHFFFAOYSA-N

InChi: InChI=1S/C19H20N4O3/c1-20-19(24)11-22-18-10-21-14-6-4-12(8-15(14)23-18)13-5-7-16(25-2)17(9-13)26-3/h4-10H,11H2,1-3H3,(H,20,24)(H,22,23)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 50 mg/mL (141.89 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:

Treatment with 0.5 μM of either KAI407 or BQR695 causes GFP-PHOsh2 to redistribute to the parasite plasma membrane, consistent with depletion of intracellular PI4P upon inhibition of PfPI4K function. BQR695 shows no evidence of toxicity against mature red blood cells (RBCs), induces a schizont-stage arrest indistinguishable from that observed in imidazopyrazine-treated parasites and exhibits cross-resistance with the imidazopyrazine-resistant lines.

References:

  1. Fowler ML, et al. Using hydrogen deuterium exchange mass spectrometry to engineer optimized constructs for crystallization of protein complexes: Case study of PI4KIIIβ with Rab11. Protein Sci. 2016 Apr;25(4):826-39.
  2. McNamara CW, et al. Targeting Plasmodium PI(4)K to eliminate malaria. Nature. 2013 Dec 12;504(7479):248-253.

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

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