LP-935509

SKU: orb1308115

Description

LP-935509

Research Area

Cell Biology, Infectious Disease & Virology, Metabolism Research, Neuroscience

Images & Validation

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Key Properties

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CAS Number	1454555-29-3
MW	396.44
Purity	98.82%
Formula	C₂₀H₂₄N₆O₃
SMILES	COc1ncccc1-c1cnn2ccc(nc12)N1CCN(CC1)C(=O)OC(C)C
Target	SARS-CoV,AAK1 (AP2 associated kinase 1),Serine/threonin kinase,AAK1
Solubility	DMSO:175 mg/mL (441.43 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.09 mM)

Bioactivity

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Target IC50	AAK1:0.9 nM(Ki)\|AAK1:3.3 nM\|GAK:320 nM\|BIKE:14 nM
In Vivo	METHODS: LP-935509 (10, 30, and 60 mg/kg) was administered orally (10 ml/kg), and Von Frey tests were performed at 0, 30, and 120 min after administration. RESULTS Oral administration of LP-935509 resulted in a dose-dependent reduction in phase II paw withdrawal that was significantly lower than that in vehicle-treated animals (Figure 3A). In particular, 30 mg/kg and 60 mg/kg of LP-935509 resulted in a significant reduction in pain behavior. Read more...
In Vitro	METHODS: The effects of LP-935509 on the activities of the two most closely related kinases, BIKE and GAK kinases, were evaluated; the ability of 1 μM LP-935509 to inhibit the binding of 389 kinases to ATP-binding probes was measured. RESULTS LP-935509 is a potent inhibitor of BIKE (IC50= 14 nM) and a modest inhibitor of GAK (IC50= 320 ± 40 nM), and LP-935509 inhibited the binding of more than 70% of the probes to 13 kinases, including BIKE. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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GAK, formalin, LP 935509, LP935509, LP-935509, inhibit, Inhibitor, infection, orally active, pain, Cyclin G-associated Kinase (GAK), cyclin G-associated kinase (GAK), chronic constriction injury, Adaptor-associated Kinase 1, AAK1, AAK1 (AP2 associated kinase 1), AAK1(AP2associatedkinase1), Antinociceptive, AP2 associated kinase 1, AP2associatedkinase1, AP2-associated kinase 1, ATP-competitive, Auxilin 2, BIKE, brain-penetrant, streptozotocin, spinal nerve ligation, SNL, SARS-CoV, SARS coronavirus, threoninkinase, Serine kinase, Serinekinase, threonin kinase

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Compound Identifiers

PubChem CID

86697436 ↗

Key Properties

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No computed properties available.

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LP-935509 (orb1308115)

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LP-935509

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

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Protocol Information

LP-935509 (orb1308115)

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