cancers

ML-180 (SR1848) is a potent inverse agonist of the orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) with an IC50 of 3.7 μM.

Mevociclib (SY-1365) is a highly selective covalent inhibitor of CDK7, possessing therapeutic potential in both hematological and solid tumors.

PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM).

COH-SR4 (COH-SR4 (Mitochondria uncoupler SR4)) is a uncoupler of mitochondrial oxidative phosphorylation. COH-SR4 modulates amp-dependent kinase (ampk)-mammalian target of rapamycin (mtor) signaling, and inhibiting proliferation of hepg2 hepatocarcinoma cells

653-47 hydrochloride is a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. It is also a very weak CREB inhibitor with IC50 of 26.3 μM.

Afamelanotide acetate is a synthetic α-melanocyte stimulating hormone analogue and first-in-class melanocortin-1 receptor agonist, used to for Erythropoietic Protoporphyria.

Melanotan I is a non-specific melanocortin receptor (MCR) agonist, an α-melanocyte-stimulating hormone (α-MSH) analog, which is injected subcutaneously to increase the amount of melanin in the skin Melanotan I is used as an adjunct to tanning Melanotan I has been used for the prevention of sunlight-induced skin cancers Melanotan I has been used in the study of melanoma and for male erectile dysfunction Melanotan I may be used to prevent sun-induced skin cancer and may be used to study melanoma and male erectile dysfunction.

ML239 (CID-49843203) is a potent and selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 μM.

Avelumab is a humanized anti-PD-L1 monoclonal antibody that binds to PD-L1 with high specificity (Kd = 0.1 nM) and exhibits potential antibody-dependent cell-mediated cytotoxicity (ADCC). Avelumab exerts a dual mechanism of action, combining direct antitumor activity with ADCC. Avelumab is used in research on cancers such as Merkel cell carcinoma.

Rituximab is an anti-CD20 chimeric monoclonal antibody used to study certain autoimmune diseases and cancers.

Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.

Ondansetron hydrochloride dihydrate (GR 38032) is a competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

Zoldonrasib (RMC-9805) is a mutant-selective covalent KRAS G12D inhibitor with oral activity and significant antitumor activity, inducing tumor cell apoptosis in preclinical models of various KRAS-mutant cancers.

Cyclophosphamide is an alkylating agent type of anti-tumor drug, and its main target is DNA. Cyclophosphamide inhibits the proliferation of tumor cells by undergoing alkylation reactions with DNA, interfering with the replication and transcription processes of DNA.

Linsitinib (OSI-906) belongs to small molecule inhibitors and is a dual IGF-1/IR inhibitor (IC50 = 35 and 75 nM, respectively) with selectivity, cell permeability, and oral activity. This compound is used in antitumor research and can effectively inhibit cell proliferation and induce apoptosis.

Zavondemstat (QC8222) is an orally active, selective inhibitor of the histone lysine demethylase 4 (KDM4) family, with an IC₅₀ of ≤ 0.08 μM against human KDM4A–D and a K₊₀ of 0.52 μM against human KDM4C. Zavondemstat activates tumor suppressor genes, induces apoptosis, causes S-phase cell cycle arrest, and inhibits cancer cell proliferation. In in vivo studies, Zavondemstat inhibits tumor growth and induces tumor regression. Zavondemstat can be used in cancer research.

HRO761 (Werner syndrome RecQ helicase-IN-1, Example 42) is a small molecule inhibitor, a potent WRN inhibitor with high efficacy, and can be used for research on cancers such as colon cancer and gastric cancer.

Cadonilimab (AK104) is a tetravalent PD-1/CTLA-4 bispecific humanised antibody that activates T cells by enhancing IL-2 and IFN-γ secretion while reducing pro-inflammatory cytokine secretion (e.g., IL-6, IL-8). It offers low toxicity and high affinity, making it suitable for metastatic cervical, gastric, hepatic, and pulmonary cancers, pancreatic cancer, and oesophageal squamous cell carcinoma.

Enfortumab is a monoclonal antibody against Nectin-4.Enfortumab can be used to synthesize antibody-drug couplings (enfortumab vedotin) and can also be used in conjunction with platinum compounds to study uroepithelial cancers.

STX-478 is an orally active and selective PI3Kα inhibitor that penetrates the blood-brain barrier and has anticancer activity to inhibit tumor growth.STX-478 is indicated for the study of breast cancer and other cancers.

RLY-2608 is a small molecule inhibitor, a selective allosteric PI3Kα inhibitor with high selectivity for PIK3CA mutations. This compound effectively inhibits tumor growth in PIK3CA-mutant xenograft models and is primarily used for research on PIK3CA-driven cancers.

Calderasib (MK-1084) is a selective KRAS G12C inhibitor with an IC50 value of 1.2 nM . Calderasib (MK-1084) exhibits significant anticancer activity, and it can be employed either as a monotherapy or in combination with the PD-1 inhibitor Pembrolizumab, providing a versatile approach for the investigation of KRAS-mutant driven cancers.

Divarasib (GDC-6036) is an investigational, oral, high-potency and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib irreversibly locks KRAS G12C oncoprotein in an inactive state and inhibits tumor cell growth. It is being investigated for use in solid tumors, including non-small cell lung and colorectal cancers and other types of cancer.