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APY 29

Names

[ CAS No. ]:
1216665-49-4

[ Name ]:
APY 29

[Synonym ]:
2,4-Pyrimidinediamine, N-1H-benzimidazol-5-yl-N-(3-cyclopropyl-1H-pyrazol-5-yl)-
N2-1H-Benzimidazol-6-yl-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine
N-(1H-Benzimidazol-5-yl)-N-(3-cyclopropyl-1H-pyrazol-5-yl)-2,4-pyrimidinediamine

Biological Activity

[Description]:

APY29 is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation with IC50 of 280 nM and activates IRE1α RNase activity.

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> IRE1
Research Areas >> Cancer

[Target]

IC50: 280 nM (IRE1α)


[In Vitro]

APY29 divergently modulates the RNase activity and oligomerization state of IRE1α. APY29 is exerting their opposing effects on RNase activity through the same binding site. APY29 divergently affects IRE1α oligomerization. APY29 demonstrates opposing dose-dependent effects on ER stress-induced activation of the RNase of endogenous IRE1α[1].

[References]

[1]. Wang L, et al. Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors. Nat Chem Biol. 2012 Dec;8(12):982-9.


[Related Small Molecules]

STF-083010 | 4μ8C | KIRA6 | MKC3946 | GSK2850163 | MKC9989 | MKC8866 | NSC95682 | B I09

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
782.3±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C17H16N8

[ Molecular Weight ]:
332.362

[ Flash Point ]:
426.9±35.7 °C

[ Exact Mass ]:
332.149780

[ PSA ]:
107.20000

[ LogP ]:
1.66

[ Vapour Pressure ]:
0.0±2.7 mmHg at 25°C

[ Index of Refraction ]:
1.861

[ Storage condition ]:
2-8℃

Related Compounds