Antitumor

Antitumor agent-19 is a modulator of tumor-associated macrophages with EC50s of 17.18 μM and 18.87 μM in the RAW 264.7 cells and the BMDM cells.

Antitumor agent-4 is a butenylphenyl phosphate derivative, is an agent of mammary cancer and anovulatory sterility.

Antitumor agent-3, a potent compound, comprises a novel imidazopyridine with excellent antitumor activity as its active ingredient.

Antitumor agent-21 (TRX818) is an orally bioavailable agent with potential antineoplastic and anti-vasculogenic mimicry (VM) activities.

Antitumor agent-28 is a compound that specifically targets and inhibits the activity of the ataxia telangiectasia mutated (ATM) kinase. By doing so, it effectively impedes the progression of ATM-mediated diseases and demonstrates significant anti-cancer activity.

Antitumor agent-23 exhibits potent antitumoral activity, as demonstrated by its GI50 values of 38, 48, 5, 27, 80, and 28 nM against the lymphoma cell lines GRANTA-519, KARPAS-422, KARPAS-299, RAMOS, DAUDI, and RAJI respectively.

Antitumor agent-2 has anti-inflammatory and anti-tumor activity and can be used to study cancer.

BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction.

AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.

Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an aromatic diamidine agent effective against various microorganisms, including protozoa (Trypanosoma brucei, Leishmania spp., and Babesia spp.) and fungi (Pneumocystis jirovecii). It is a potent and selective inhibitor of protein tyrosine phosphatases and phosphatase of regenerating liver. Pentamidine dihydrochloride inhibits the parasite Leishmania infantum with an IC50 of 2.5 μM.

AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages. AKB-6899 leads to stabilization of HIF-2α which induces sVEGFR-1 production from tumor-associated macrophages and decreases tumor growth.

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.

Tubulin inhibitor 24 is a potent compound that inhibits tubulin polymerization.

K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 µM and Ki of 6.4 µM. K145 hydrochloride can induce apoptosis and has strong antitumor activity.

Mitoxantrone dihydrochloride (NSC-301739) is the hydrochloride salt of an anthracenedione antibiotic with antineoplastic activity. It is a type II topoisomerase inhibitor.

Erythromycin (E-Mycin) is a Macrolide and Macrolide Antimicrobial. The physiologic effect of erythromycin is by means of Decreased Sebaceous Gland Activity.

Hesperidin (Cirantin) is a flavanone glycoside found in citrus fruits with antioxidant, anti-inflammatory, anti-carcinogenic, and antihypertensive and lipid-lowering activity.

Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen.

Mycophenolic acid (Mycophenolate) is an inosine monophosphate dehydrogenase(IMPDH) inhibitor with anti-proliferative activity.

Dasatinib (BMS-354825) is an orally active, ATP-competitive tyrosine kinase inhibitor that targets Src and Bcr-Abl (Ki=16/30 pM), with antitumor activity, used in the treatment of leukemia and lymphoma.

Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.

Nilotinib (AMN107) is a Bcr-Abl tyrosine kinase inhibitor with oral activity. Nilotinib has antitumor activity and may be used for the treatment of Imatinib-resistant chronic myelogenous leukemia (CML).

Nilotinib monohydrochloride monohydrate (Nilotinib (monohydrochloride monohydrate)) is significantly potent BCR-ABL against, is a second generation tyrosine kinase inhibitor (TKI), and is active against many BCR-ABL mutants.

Genipin ((+)-Genipin), an active aglycone derived from an iridoid glycoside called geniposide, is found in the fruit of Gardenia jasminoides Ellis.