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LX2343

  Cat. No.:  DC10754   Featured
Chemical Structure
333745-53-2
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More than 5000 active chemicals with high quality for research!
Field of application
LX-2343 is a novel non-ATP competitive PI3K inhibitor, negatively regulating AKT/mTOR signaling, thus promoting autophagy, and increasing A-beta clearance.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 333745-53-2
Chemical Name: LX2343
Synonyms: LX2343
SMILES: C1=C(NC(CN(C2=CC(Cl)=CC=C2OC)S(C2=CC=CC=C2)(=O)=O)=O)C=C2OCOC2=C1
Formula: C22H19ClN2O6S
M.Wt: 474.912
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance.
In Vivo: APP/PS1 mice express chimeric human Swedish mutant APP and a mutant human presenilin 1 protein and are widely used as an effective animal model for AD dementia. The amelioration of memory impairment by LX2343 is evaluated t in this model using the MWM test. In 8-d training trials, the path lengths and escape latencies used to find the platform for APP/PS1 transgenic mice are remarkably longer than those for non-transgenic mice, while 10 mg/kg LX2343 administration obviously antagonizes the prolonged path lengths and escape latencies at d 7 and 8. In the probe trial assay, the LX2343-administered transgenic mice cross over the hidden location of the platform more frequently compared with the vehicle-administered transgenic mice[1].
In Vitro: LX2343 (5-20 μM) dose-dependently decreased Aβ accumulation in HEK293-APPsw and CHO-APP cells, and promotes Aβ clearance in SH-SY5Y cells and primary astrocytes. LX2343 ameliorates cognitive dysfunction in APP/PS1 transgenic mice via both Aβ production inhibition and clearance promotion, which highlights the potential of LX2343 in the treatment of AD. Western blot results in both HEK293-APPsw cells and CHO-APP cells demonstrate that LX2343 fails to regulate BACE1 protein levels, while in vitro BACE1 enzymatic activity assays indicated that LX2343 dose-dependently decreases BACE1 activity (TDC as a positive control) with an IC50 of 11.43±0.36 μM. To test whether competition exists between LX2343 and ATP, we investigated the effects of ATP at different concentrations on the inhibitory activity of LX2343. The result demonstrated that the inhibition of LX2343 against PI3K is virtually unaffected by ATP. Thus, this result suggested that LX2343 is a non-ATP competitive inhibitor of PI3K. In the presence of 10 μM of ATP, the IC50 of LX2343 is 13.11±1.47 μM, in the presence of 50 μM ATP, the IC50 of LX2343 is 13.86±1.12 μM, in the presence of 100 μM ATP, the IC50 of LX2343 is 15.99±3.23 μM [1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC71172 NVP-CLR457 NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity.
DC70705 PQR514 PQR514 is a potent selective pan-PI3K inhibitor with binding Ki of 2.2 and 33 nM for p110α and mTOR, repectively.PQR514 inhibits phosphorylated S6 ribosomal protein (pS6, Ser235/236) and phosphorylation PKB Ser473 in A2058 cells with IC50 of 17 and 68 nM, respectively.PQR514 displays negligible interference with protein kinase activities at 10 uM in a KINOMEScan panel.PQR514 exhibits growth inhibition in vitro across a panel of 66 tumor cells with GI50 of 0.25 uM.PQR514 demonstrates significant antitumor activity aginst OVCAR-3 human ovarian cancer xenograft model in BALB/c nude mice.
DC44213 PF-06843195 PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.
DC7228 PF-04691502 PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK.
DC1068 XL147 analogue(PI3K inhibitor X) XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for wild type and mutant p110α with IC50 of 40 nM and 40 nM, respectively.
DC10019 VPS34 inhibitor 1 (Compound 19, PIK-III analogue) VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.
DC8884 Voxtalisib (XL765, SAR245409) Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR.
DC5181 Voxtalisib Analogue Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR.
DC9311 Serabelisib(TAK-117,INK1117,MLN1117) TAK-117(INK1117,MLN1117) is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity.
DC10140 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K and BRD4with IC50 values of 16 and 241 nM for PI3Kα and BD1, respectively.
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