Description
BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.
Product information
CAS Number: 2101517-69-3
Molecular Weight: 533.44
Formula: C23H15F8N3OS
Chemical Name: (2R)-2-({[3,5-bis(trifluoromethyl)phenyl]carbamothioyl}amino)-N-(2,4-difluorophenyl)-2-phenylacetamide
Smiles: O=C(NC1=CC=C(F)C=C1F)[C@H](NC(=S)NC1C=C(C=C(C=1)C(F)(F)F)C(F)(F)F)C1C=CC=CC=1
InChiKey: BDBWQANRZRCMMD-LJQANCHMSA-N
InChi: InChI=1S/C23H15F8N3OS/c24-15-6-7-18(17(25)11-15)33-20(35)19(12-4-2-1-3-5-12)34-21(36)32-16-9-13(22(26,27)28)8-14(10-16)23(29,30)31/h1-11,19H,(H,33,35)(H2,32,34,36)/t19-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 250 mg/mL (468.66 mM).
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:
BL-918 (compound 33i) binds to ULK1 with a high binding affinity (KD=0.719 μM). BL-918 (5 μM; for 24 hours) induces autophagy in Neuron-Like SH-SY5Y cells. BL-918 (0.5-50 μM; for 24 hours) can partially reverse MPP+-induced cell death, which is determined by enhancing cell viability. BL-918 (5 μM; for 6-36 hours) time-dependently elevates the expression levels of LC3-II, Beclin-1, and its phosphorylation status, whereas reduces the level of the selective autophagy substrate SQSTM1/p62. BL-918 elevates Ser317 and Ser555 phosphorylation of ULK1, as well as decreases Ser757 phosphorylation of ULK1.
In Vivo:
BL-918 (compound 33i; 20, 40, or 80 mg/kg/day; oral gavage; began 2 days before the first injection of saline/MPTP and continuously maintained for 5 days after the last injection of saline/MPTP) attenuates the loss of DA and its metabolites. BL-918 obviously decreases the levels of dopamine (DA), 3,4-dihydroxyphenylacetic acid (DOPAC), and homovanillic acid (HVA).
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.