AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
RSK-IN-1 (compound 7d) is a RSK inhibitor that inhibits the YB-1 phosphorylation. RSK-IN-1 has anti-tumor effects[1].
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively)[1].
PF-4708671 is a potent cell-permeable S6K1 inhibitor with a Ki of 20 nM and IC50 of 160 nM.
AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
Bupivacaine Hydrochloride is a local anaesthetic drug belonging to the amino amide group.Target: OthersBupivacaine hydrochloride is an effective local anesthetic agent. It has a rapid onset time, a high frequency of surgical anesthesia, a long duration, and a low incidence of side effects [1]. Median doses of bupivacaine (in milligrams per kilogram) producing asystole in protocol 1 were for 17.7 for saline, 27.6 for 10% Intralipid, 49.7 for 20% Intralipid, and 82.0 for 30% Intralipid (P < 0.001 for differences between all groups). Differences in mean +/- SE concentrations of bupivacaine in plasma (in micrograms per milliliter) were significant (P < 0.05) for the difference between saline (93.3 +/- 7.6) and 30% Intralipid (212 +/- 45). In protocol 2, lipid infusion increased the dose of bupivacaine required to cause death in 50% of animals by 48%, from 12.5 to 18.5 mg/kg. The mean lipid:aqueous ratio of concentrations of bupivacaine in a plasma-Intralipid mixture was 11.9 +/- 1.77 (n = 3) [2].
LJH685 is a potent , specific and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50 of 4 to 13 nM.IC50 value: 4 to 13 nM [1]Target: RSKin vitro: LJH685 efficiently inhibits RSK activity in cells. LJH685 RSK inhibition correlates with antiproliferative effects in MAPK pathway-dependent cancer cell lines only in anchorage-independent growth setting. The EC 50 values of LJH685 is 0.73 and 0.79 μM in MDA-MB-231 and H358. [1]
SL 0101-1 (SL0101), a kaempferol glycoside, isolated from the tropical plant F. refracta, is a cell-permeable, selective, reversible, ATP-competitive p90 Ribosomal S6 Kinase (RSK) inhibitor, with an IC50 of 89 nM. Shows proliferation inhibition in human breast cancer cell line MCF-7 and produces a cell cycle block in G1 phase[1].
AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.