SOS1-IN-10 is a potent SOS1 inhibitor with an IC50 of 13 nM for KRAS G12C-SOS1 (WO2022017519A1, compound 8).

SOS1-IN-9 is a potent SOS1 inhibitor with an IC50 of 116.5 nM for SOS1-KRAS G12C (WO2022028506A1, compound 302).

SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAFwt, and bRAFV600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively.

RAF-IN-1 is a potent b/cRAF inhibitor with an IC50s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAFwt, and bRAFV600E. RAF-IN-1 shows cell growth inhibition with GI50s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAFV600E mutation, respectively.

RMM-46 is a selective and reversible covalent inhibitor for MSK/RSK-family kinases.

HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM), HPK1-IN-21 also has orally active.

Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research.

Immunoproteasome inhibitor 1 is a potent, reversible, time-independent immunoproteasome and proteasome inhibitor (Kis of 1.18, 0.27, 1.91 μM in β5c, β1i, β5i submits, respectively). Immunoproteasome inhibitor 1 can be used for the treatment of certain neoplastic diseases.

PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas.

Dihydroeponemycin, an analogue of the antitumor and antiangiogenic natural product eponemycin, selectively targets the 20S proteasome. Dihydroeponemycin covalently modifies a subset of catalytic proteasomal subunits, binding preferentially to the IFN-gamma-inducible subunits LMP2 and LMP7. Dihydroeponemycin-mediated proteasome inhibition induces a spindle-like cellular morphological change and apoptosis.

PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis.

PI3K-IN-29 is a potent PI3K inhibitor. PI3K-IN-29 displays good inhibition potencies against U87MG, HeLa and HL60 cells with IC50 values of 0.264, 2.04 and 1.14 µM, respectively. PI3K-IN-29 inhibits PI3K/Akt pathway by inhibiting phosphorylation of Akt that is catalyzed by PI3K.

PI3K-IN-27 is a potent inhibitor of PI3K. PI3K belongs to a large family of lipid signaling kinase that plays key role in cellular process including cell growth, differentiation, migration and apoptosis. PI3K-IN-27 has the potential for the research of hyper-proliferative diseases like cancer and inflammation, or immune and autoimmune diseases (extracted from patent WO2021233227A1, compound 1).

PI3K-IN-30 (compound 6d) is a potent PI3K inhibitor with IC50s of 5.1, 136, 30.7 and 8.9 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.

PI3Ka-IN-5 (compound 6 ab) is a potent PI3Kα/mTOR inhibitor, with an IC50 of 0.7 nM and 3.3 nM, respectively. PI3Ka-IN-5 can be used for the research of colorectal cancer.

PHGDH-IN-2 is a potent and NAD+ competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells.

GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity.

GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity.

Anti-inflammatory agent 12 (Compound 2) is a pentacyclic triterpene compound. Anti-inflammatory agent 12 shows a significant bias in the LPS-induced inflammatory response with an IIC50 value of 2.22 μM. Anti-inflammatory agent 12 has the potential for the research of inflammation disease.

ZL-Pin13 is a high potent cell-active covalent inhibitor targeting the Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) with an IC50 of 67 nM. ZL-Pin13 effectively inhibits the proliferation and downregulated the Pin1 substrates in MDA-MB-231 cells.

Anticancer agent 33 (compound 3), a Squamocin and Bullatacin derivative, is a potent anticancer agent. Anticancer agent 33 shows high potency to inhibit 4T1 breast cancer cell line (A549, HeLa, HepG2 and MCF-7 cells) growth with IC50s of 1.9-5.4 µM.

AGL-0182-30 is a proprietary microtubule disrupting agent.

BOD-NH-NP is an activatable fluorescent probe for imaging endogenous nitric oxide via the eNOS enzymatic pathway.

Antitumor agent-47 (Compound 3e) is a silibinin derivative with an antitumor activity. Antitumor agent-47 shows cytotoxic activity against NCI-H1299 and HT29 cells with IC50 values of 8.07 µM and 6.27 µM, respectively.

Antitumor agent-49 (Compound 10) is a Harmine derivative-furoxan hybrids containing NO donor, with antitumor activities. Antitumor agent-49 shows cytotoxic activity against HepG2 cells with an IC50 of 1.79 µM. Antitumor agent-49 produces high levels of NO in vitro.

TS010 is a potent inhibitor of GLO-I with IC50 of 0.57 μM. TS010 has the potential for the research of cancer disease.

ChemR23-IN-3 is a potent thiazole-based ChemR23 inhibitor with an IC80 value of 12 nM.

17β-HSD1-IN-1 (Compound 1) is a highly selective 17β-HSD1 inhibitor with IC50s of 5.6 and 3155 nM for 17β-HSD1 and 17β-HSD2, respectively. 17β-HSD1-IN-1 can be used for the research of non-small cell lung cancer (NSCLC).

BSc5367 is a potent Nek1 inhibitor with an IC50 of 11.5 nM. NIMA-related protein kinase Nek1 is crucially involved in cell cycle regulation, DNA repair and microtubule regulation and dysfunctions of Nek1 play key roles in amyotrophic lateral sclerosis (ALS), polycystic kidney disease (PKD) and several types of radiotherapy resistant cancer.

PKN1/2-IN-1 is a potent, cell penetrant and selective PKN2 (PRK2) inhibitor (IC50=16 nM; Ki=8 nM).