LP-935509_product_DataBase

Bioactivity

LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research[1].

Target

IC50: 3.3 ± 0.7 nM (AAK1), 14 nM (BIKE), 320 ± 40 nM (GAK)

Invitro

LP-935509 inhibits μ2 phosphorylation with an IC50 value of 2.8 ± 0.4 nM, inhibits phosphorylation of a peptide derived from the μ2 protein with an IC50 value of 3.3 ± 0.7 nM[1].LP-935509 exhibits a dose-dependent inhibition of the SARS-CoV-2 S-RBD internalization into host cells[2].

In Vivo

LP-935509 (0-60 mg/kg; PO, single) causes a robust reduction in pain behavior[1].LP-935509 (0.1-30 mg/kg; PO, single dosage) causes a dose-dependent reversal of thermal hyperalgesia in CCI model[1].LP-935509 (IV (1 mg/kg) or orally (10 mg/kg); once) has 100% oral bioavailability and a plasma half life of 3.6 hours[1]. Animal Model:

Name

LP-935509

CAS

1454555-29-3

Formula

C20H24N6O3

Molar Mass

396.44

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Kostich W, et al. Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain. J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. [2]. Mushtaq, et al. Role Of Endocytic Machinery Regulators in EGFR Traffic and Viral Entry (2021). Theses & Dissertations. 532.

PeptideDB

LP-935509

CAS: 1454555-29-3 F: C20H24N6O3 W: 396.44