All Photos(1)
Synonym(s):
T-00127-HEV1, 3-(3,4-Dimethoxyphenyl)-2,5-dimethyl-N-(2-morpholinoethyl)pyrazolo[1,5-a]pyrimidin-7-amine, PI4KIIIβ Inhibitor II
Empirical Formula (Hill Notation):
C22H29N5O3
Recommended Products
Assay
≥95% (HPLC)
Quality Level
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
A cell-permeable pyrazolopyrimidinamine derived enviroxime-like compound that displays anti-poliovirus activity with broad specificity for enteroviruses (EC50 = 0.77, 3.38, 2.5, 1.03 & >44 µM for PV, CVB3, HRVM, HCV 1b & HCV 2a, respectively). Dose-dependently inhibits viral RNA replication. Acts as a potent, selective, ATP-competitive and reversible inhibitor of PI4KIIIβ (IC50 = 150 nM) with poor affinity towards PI4KIIIα & PI4KIIα (IC50 = ~75 & ≥100 µM). Shown to cause PI4KIIIβ accumulation and reduce PI4P at the Golgi apparatus. Exhibits low cytotoxicity (CC50 >50 µM in HeLa cells) and attractive PK profile in mice. PI4KIIIβ Inhibitor I, BF738735 (Cat. No. 533657) is also available.
A cell-permeable pyrazolopyrimidinamine derived enviroxime-like compound that displays anti-poliovirus activity with broad specificity for enteroviruses (EC50 = 0.77, 3.38, 2.5, 1.03 & >44 µM for PV, CVB3, HRVM, HCV 1b & HCV 2a, respectively). Dose-dependently inhibits viral RNA replication. Acts as a potent, selective, ATP-competitive and reversible inhibitor of PI4KIIIβ (IC50 = 150 nM) with poor affinity towards PI4KIIIα & PI4KIIα (IC50 = ~75 & ≥100 µM). Shown to cause PI4KIIIβ accumulation and reduce PI4P at the Golgi apparatus. Exhibits low cytotoxicity (CC50 >50 µM in HeLa cells) and attractive PK profile in mice. PI4KIIIβ Inhibitor I, BF738735 (Cat. No. 533657) is also available.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PI4KIIIβ
PI4KIIIβ
Reversible: yes
Target IC50: 150 nM for PI4KIII&beta
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Mejdrova, I., et al. 2015. J. Med. Chem.58, In press.
Spickler, C., et al. 2013. Antimicrob. Agents Chemother.57, 3358.
Sasaki, J., et al. 2012. EMBO J.31, 754.
Arita, M., et al. 2011. J. Virol.85, 2364.
Spickler, C., et al. 2013. Antimicrob. Agents Chemother.57, 3358.
Sasaki, J., et al. 2012. EMBO J.31, 754.
Arita, M., et al. 2011. J. Virol.85, 2364.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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