LRE1

Names

[ Name ]:
LRE1

[Synonym ]:
MFCD23150321
6-Chloro-N4-cyclopropyl-N4-(3-thienylmethyl)-2,4-pyrimidinediamine
2,4-Pyrimidinediamine, 6-chloro-N4-cyclopropyl-N4-(3-thienylmethyl)-

Biological Activity

[Description]:

A novel potent, specific and allosteric soluble adenylyl cyclase (sAC) inhibitor with IC50 of 3.3 uM in RF-MSS assays; does not inhibit other transmembrane adenylyl cyclases (tmACs) indluding tmACs I, II, V, VIII and IX at 50 uM; binds to the bicarbonate activator binding site and inhibited sAC via a unique allosteric mechanism; inhibits cAMP accumulation in 4-4 cells with an IC50 of 11 uM, and is non-toxic and does not uncouple mitochondria.

[References]

References 1. Ramos-Espiritu L, et al. Nat Chem Biol. 2016 Oct;12(10):838-44. View Related Products by Target Adenylate Cyclase

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
532.6±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₂H₁₃ClN₄S

[ Molecular Weight ]:
280.776

[ Flash Point ]:
275.9±32.9 °C

[ Exact Mass ]:
280.054932

[ LogP ]:
3.79

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.744

Related Compounds

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