Lys01 trihydrochloride|cas: 1391426-24-6

Cas No.:	1391426-24-6
Synonyms:	Lys05
SMILES:	CN(CCNC1=CC=NC2=C1C=CC(Cl)=C2)CCNC3=CC=NC4=CC(Cl)=CC=C43.[H]Cl.[H]Cl.[H]Cl
Formula:	C₂₃H₂₆Cl₅N₅
M.Wt:	549.75
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Lys01, is a 10-fold more potent autophagy inhibitor than HCQ. Compared with HCQ, Lys05, a water-soluble salt of Lys01, more potently accumulates within and deacidifies the lysosome. Lys01 and lys01 trihydrochloride produce equivalent dose-dependent increases in the LC3II/LC3I ratio, accumulation of the autophagy cargo protein p62, and identical IC50 values in the MTT assay.With this high-dose, short-term treatment, no mice die, but after 2 d of dosing, mice treated with lys01 trihydrochloride 76 mg/kg i.p. are observed to have arched backs and lethargy. Morphologically, EM show that cells with intact nuclear and cytoplasmic membranes contain large AVs in lys01 trihydrochloride-treated tumors. Tumor growth is significantly impaired in lys01 trihydrochloride-treated tumors compared with controls. Lys01 trihydrochloride treatment results in a 53% reduction in the average daily tumor growth rate compared with vehicle-treated controls. A significant three- and six-fold accumulation of AV is observed at the end of 14 d of treatment in HCQ- and lys01 trihydrochloride-treated tumors, respectively, compared with control-treated tumors.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC73152	SW118150	SW120619 is a specific small molecule inhibitor of WNK3 kinase with IC50 of 0.7 uM, weakly inhibits WNK1 and WNK2 with IC50 of 2.3 and 16.8 uM, respectively.
DC73146	MK-1468	MK-1468 is a potent, selective, brain-penetrant LRRK2 inhibitor with IC50 of 0.4 nM (G2019S LRRK2), potently inhibits the phosphorylation of LRRK2 serine 935 (pSer935) in hPBMCs with IC50 of 2.8 nM.
DC73145	FX2149	FX2149 (FX 2149) is a potent, BBB permeable inhibitor of LRRK2 GTP binding activity with IC90 of 10 nM, reduces PD-linked mutant LRRK2 variants (G2019S and R1441C) that bound with GTP.
DC72873	MTK458	MTK458 (MTK-458) is a potent, selective and brain penetrant PINK1 activator, MTK-458 promotes the first step in mitophagy. MTK458 selectively activates PINK1 by stimulating dimerization and stabilization of the PINK1/TOM complex. MTK458 binds to PINK1 and stabilizes an active heterocomplex, thereby increasing mitophagy. MTK458 reduces the PINK1 substrate pS65-Ubiquitin (pUb) in primary neurons and in vivo. MTK458 drives clearance of pathologic α-synuclein in vitro and in vivo, decreases pS129 α-synuclein aggregates and normalized both brain and corresponding plasma pUb levels in both cellular and animal models of α-synuclein aggregation (PD-like pathology).
DC72558	GLPG3970	GLPG3970 (compound 88) is a first-in-class SIK2/SIK3 inhibitor. GLPG3970 can be used for the research of inflammation and autoimmune disease.
DC70343	DCC-3116	DCC-3116 (DCC3116) is a first-in-class, selective inhibitor of ULK1/2 kinases (IC50=4.7/35 nM) and autophagy.DCC-3116 is an oral ULK1/2 inhibitor targeting the autophagy pathway, a key mechanism of tumor survival and resistance to targeted therapy.
DC48117	EB-42486	EB-42486 is a novel, potent, and highly selective G2019S-LRRK2 inhibitor (IC50 < 0.2 nM).
DC46639	WH-4-025	WH-4-025 is a Salt-inducible kinase (SIK) inhibitor (WO2016023014 A2).
DC28954	Curcumin analog C1(TFEB activator 1 )	TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway an
DC10635	MRT67307 HCl	MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively.