ps6

Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.

BC1618 (2-Propanol, 1-[bis(phenylmethyl)amino]-3-[4-(trifluoromethyl)phenoxy]-) is an orally active Fbxo48 inhibitor that stimulates Ampk-dependent signaling. It promotes mitochondrial fission, promotes autophagy and improves hepatic insulin sensitivity.

Vistusertib (AZD2014) is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.

APS6-45 inhibits RAS/MAPK signaling and exhibits anti-tumor activity.

RPS6-IN-1 (Compound 22o) inhibits cell migration and induces apoptosis (increasing the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). It reduces mitochondrial membrane potential and activates autophagy (Autophagy) through the PI3K-Akt-mTOR signaling pathway, damaging mitochondria and lysosomes within the cell and causing endoplasmic reticulum stress. RPS6-IN-1 also inhibits the phosphorylation of RPS6. Notably, RPS6-IN-1 is a low systemic toxicity anticancer agent.

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.

BIX02188 is a selective and potent MEK5 inhibitor that inhibits MEK5-induced apoptosis in cells expressing the oncogenic mutant FLT3-ITD.

BIX02189 is a potent and selective inhibitor of MEK5 and ERK5 (IC50: 1.5 nM and 59 nM).

(E/Z)-BIX 02189 is an isomer of BIX 02189 that can be employed in biochemical experiments.

Ro3280 (Ro5203280) is an effective, specific inhibitor of PLK1(IC50=3, Kd=0.09 nM).

RMC-5552 is a potent and selective inhibitor of mTORC1 that blocks phosphorylation of downstream signaling targets pS6K and p4EBP1 with IC50 values of 0.14 nM and 0.48 nM, respectively. RMC-5552 shows markedly reduced inhibition of pAKT (IC50 19 nM), achieving approximately 40-fold selectivity for mTORC1 over mTORC2. RMC-5552 has demonstrated anticancer activity, supporting its potential use as a therapeutic agent in oncology and as a research tool for dissecting mTOR signaling pathways.

PQR530 is a highly potent dual pan-PI3K/mTORC1/2 inhibitor. PQR530 inhibited protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235/236) phosphorylation with IC50 values of 0.07 μM. It also showing antitumor activity.

BTX-6654 is a cereblon-based bifunctional SOS1 PROTAC degrader. This compound exhibits antiproliferative activity against cells with various KRAS mutations by reducing the expression of downstream signaling markers pERK and pS6.

DQ661 is a potent inhibitor of PPT1 and a dimeric quinacrine autophagy (autophagy) inhibitor. It effectively suppresses the activity of mTORC1 and reduces protein expression levels of pS6K T389 and pS6 S240-244. Additionally, DQ661 exhibits anticancer properties.

BTX-7312 is a cereblon-based SOS1 bifunctional degrader and acts as a molecular glue (molecular glue). It reduces downstream signaling markers pERK and pS6 and demonstrates antiproliferative activity in cells with various KRAS mutations.

KRAS ligand 4 (Compound 2) is a dual-functional molecular glue degrader based on SOS1. It reduces downstream signaling markers pERK and pS6, and exhibits antiproliferative activity in cells with various KRAS mutations.

PIM-IN-1 is a pan-PIM kinase inhibitor with an EC50 of 61 nM in KG-1 and an EC50 of 71 nM in pS6.

PF-05139962 is a novel potent mTOR inhibitor with excellent mTOR biochemical inhibition, cellular potency, kinase selectivity and in vitro ADME properties. PF-05139962 has pS473 and pS6 cellular IC50 = 48 and 6 nM respectively. PF-05139962 has great selectivity against other receptors and kinases. No genotoxicity was observed on this compound and no more than 25% inhibiton was observed for major CYP enzymes (3A4, 1A2, 2C9, 2D6) at 3 uM. This compound has LE = 0.35 and LipE up to 6.8 which is in a very desirable range for a kinase inhibitor.

mTOR inhibitor-11 (Compound 9) is a brain-penetrant compound that inhibits mTOR with an IC50 of 21 nM for pS6 and exhibits inhibitory activity against pCHK1 and PDE4D with IC50 values of 17.2 μM and 17.0 μM, respectively. This compound is utilized in CNS disease research [1].