PI3K/Akt/mTOR Signaling

HER2-IN-21 (compound 657994) is an inhibitor of the human epidermal growth factor receptor 2 (HER2) with an IC50 value of 3.85 μM.

GSK-3β inhibitor26 (Compound D14) is a GSK-3β inhibitor with an IC50 of 18.23 μM. This compound is applicable in research related to cancer, inflammation, and neurodegenerative diseases.

EGFR-IN-147 (compound ID-5841161) is a potent EGFR inhibitor, demonstrating a 14% inhibition rate at a concentration of 1μM. It holds promise for cancer research applications.

GSK3β-IN-2 (Compound S01) is an inhibitor of GSK3β with an IC50 of 0.35 nM. It activates the Wnt/β-catenin signaling pathway, promoting neurogenesis and neurite outgrowth. GSK3β-IN-2 reduces tau protein phosphorylation induced by Aβ at the Ser396 site, thereby decreasing neurofibrillary tangles. Furthermore, GSK3β-IN-2 improves Alzheimer's disease symptoms in a zebrafish model.

5-Bromo-3-indoxylacetate acts as an inhibitor of GSK-3, with a pIC50 value of 3.39.

NU5455 is a potent DNA-PKcs inhibitor, oral, boosts doxorubicin in liver tumors, amplifies topoisomerase inhibitors, no adverse effects.

EG31 is an EGFR inhibitor that effectively suppresses the proliferation of triple-negative breast cancer (TNBC) cells by inhibiting the EGFR signaling pathway. It demonstrates a GI50 value of 498.90 nM for MDA-MB-231 cells and 740.73 nM for Hs578T cells, while also inducing apoptosis. Additionally, EG31 retains its antiproliferative activity against 5-fluorouracil (5-FU) resistant TNBC cells, with a GI50 of 519.5 nM. EG31 is applicable in research on TNBC resistance.

DNA-PK-IN-9 (YK6) is a potent DNA-PK inhibitor with an IC50 of 10.47 nM, important in cancer research.

PI3K-IN-23 is a (E)-9-oxooctadec-10-en-12-ynoic acid analogue that promotes glucose uptake (EC50: 7.00 μM).

BAY-091 is a novel potent and highly selective PIP4K2A kinase inhibitor.

SIK2/3-IN-1 (Compound 7S) is an orally active and selective inhibitor of SIK2/3. It significantly inhibits tumor growth without causing weight loss in the MV4-11 AML mouse CDX model. SIK2/3-IN-1 is applicable for research in MEF2C-dependent acute myeloid leukemia.

Lys(CO-C3-p-I-Ph)-O-tBu, a pharmacokinetic modifier (PK modifier), enhances the pharmacokinetic properties of PSMA ligand molecules by increasing their residence time in plasma through improved binding to albumin and reducing absorption by the salivary glands, potentially extending the active compound's half-life. Moreover, Ac-PSMA-trillium is an effective PSMA-targeting compound for various biological applications when modified with different radioactive isotopes. When labeled with 111 In, it serves as a DOTA chelating agent and imaging agent. Alternatively, when labeled with 225 Ac, it acts as a Macropa chelator for targeted radionuclide therapy (TRT) in researching metastatic castration-resistant prostate cancer (mCRPC) [1] [2].

SIK2-IN-3 is an orally active selective inhibitor of SIK1/2 with IC50 values of 0.128/0.084 μM. It hinders the phosphorylation of CRTC3 and suppresses the production of pro-inflammatory factors in myeloid cells. Additionally, SIK2-IN-3 alleviates systemic and tissue inflammatory responses in a mouse anti-CD40 colitis model.

JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active inhibitor of EGFR with an IC 50 of 15 nM for EGFR L858R/T790M [1].

Vps34-IN-3 is a potent, selective, and orally bioavailable inhibitor of VPS34 kinase .

HER2-IN-8 is an inhibitor of HER-2 that can be used in the study of cancer and inflammation-related diseases.

EGFR-IN-160 is an EGFR inhibitor with IC50 values of 1.62, 0.49, and 0.98 μM for EGFRWT, EGFRT790M, and EGFRL858R/T790M/C797S, respectively. It can induce cell cycle arrest at the G2/M and S phases and apoptosis (Apoptosis) in NCI-H522 cells, demonstrating anticancer properties. Additionally, EGFR-IN-160 exhibits antioxidant activity against DPPH (IC50: 12.11 µM) and H2O2 (IC50: 8.89 µM).

PF-5177624 is a selective and potent PDK1 inhibitor inducing anti-tumor activity in breast cancer cells.

Vulolisib inhibits PI3K (α: IC50 0.2nM, β: 168nM, γ: 90nM, δ: 49nM), taken orally with anti-cancer properties.

EGFR-IN-38: low-toxic acrylamide-derived EGFR inhibitor, targets NSCLC, patented for research on EGFR mutation-related diseases.