GW406108X


Catalog No. Size PriceQuantity
M27875-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK.

Product information

CAS Number: 1644443-92-4

Molecular Weight: 400.21

Formula: C20H11Cl2NO4

Chemical Name: (3Z)-3-[(3,5-dichloro-4-hydroxyphenyl)methylidene]-5-(furan-2-carbonyl)-2,3-dihydro-1H-indol-2-one

Smiles: OC1C(Cl)=CC(=CC=1Cl)/C=C1/C2=CC(=CC=C2NC/1=O)C(=O)C1=CC=CO1

InChiKey: XKTUKRBLWOHYIL-MLPAPPSSSA-N

InChi: InChI=1S/C20H11Cl2NO4/c21-14-7-10(8-15(22)19(14)25)6-13-12-9-11(3-4-16(12)23-20(13)26)18(24)17-2-1-5-27-17/h1-9,25H,(H,23,26)/b13-6-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (124.93 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

GW406108X acts upon ULK1 and autophagy without affecting mTOR or AMPK activity as shown by monitoring ULK1 pS758 (mTOR site) or pS556 (AMPK site) levels. GW406108X inhibits VPS34 and AMPK with pIC50 of 6.34 (457 nM) and 6.38 (417 nM), respectively. In the presence of 5 µΜ GW406108X, the starvation-induced increase in ATG13 phosphorylation is significantly reduced. GW406108X inhibits Kif15-N420 ATPase activity by 76%.

Products are for research use only. Not for human use.

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