Bioactivity | GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM. | |||||||||
Invitro | GSK319347A (Compound 1) inhibits TBK1 enzyme with an IC50 of 93 nM, which also translates into good cell potency (72 nM). Moreover, IKK-3 Inhibitor exhibits excellent selectivity against cell-cycle kinases CDK2 and AurB[1]. IKK-3 Inhibitor (Compound 13) is a novel IκB kinase 2 (IKK2) inhibitor with an IC50 of 790 nM[2]. | |||||||||
Name | GSK319347A | |||||||||
CAS | 862812-98-4 | |||||||||
Formula | C22H19N3O5S2 | |||||||||
Molar Mass | 469.53 | |||||||||
Appearance | Solid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [1]. Johannes JW, et al. Discovery of 6-aryl-azabenzimidazoles that inhibit the TBK1/IKK-ε kinases. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1138-43. [2]. Xie HZ, et al. Pharmacophore modeling and hybrid virtual screening for the discovery of novel IκB kinase 2 (IKK2) inhibitors. J Biomol Struct Dyn. 2011 Aug;29(1):165-79. |