tumor

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC₅₀=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC₅₀=1.4 μM) and an inhibitor of CK2 (IC₅₀=98 nM). LY294002 activates apoptosis and autophagy.

MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.

PND-1186 (VS-4718) is a small molecule inhibitor, a highly specific, reversible FAK inhibitor (IC₅₀=1.5 nM) with good selectivity and cell permeability. This compound inhibits FAK phosphorylation, blocking tumor cell survival, proliferation, migration, and angiogenesis, and is primarily used for anti-tumor research on solid tumors.

MMP-9-IN-1 is an inhibitor of specific matrix metalloproteinase-9 (MMP-9).

MSA-2 is an orally available non-nucleotide STING agonist. The non-covalent dimer of MSA-2 binds to STING with nanomolar affinity. It shows anti-tumor activity in syngeneic mouse tumor models, synergizes with anti-PD-1, stimulates tumor secretion of interferon-β, induces tumor regression, and has long-lasting anti-tumor immunity. ^[3]

Talmapimod (SCIO-469) is a selective, orally active, ATP-competitive p38α inhibitor with IC₅₀ values of 9 nM for p38α and 90 nM for p38β. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.

Pyrazoloacridine (PD 115934) is a nucleic acid binding agent that inhibits the activity of topo I and II with an IC₅₀ of 1.25 μM in K562 cells. Pyrazoloacridine shows anti-cancer activity.

PACMA 31 is an irreversible and covalent inhibitor of protein disulfide isomerase (PDI) with an IC₅₀ of 10 μM. PACMA 31 significantly suppresses ovarian tumor growth and exhibits tumor targeting ability.

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

Refametinib (RDEA119) (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1/2 (IC₅₀: 19/47 nM).

AG-270 is an allosteric and orally active inhibitor of MAT2A.

4SC-203 is a multi-kinase inhibitor with potential anti-tumor activity. 4SC-203 exhibits unique selectivity for Flt3, Flt3 mutants, Axl, Alk, Fak, VEGF-R2, and Trk receptors in the low nM range.

Erlotinib (NSC-718781) is an EGFR inhibitor (IC₅₀: 2 nM). It is used for the treatment of non-small cell lung cancer.

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

Adapalene (CD271) is a dual RAR and RXR agonist, utilized in the treatment of skin conditions.

Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5).

Nortriptyline hydrochloride (ELF-101 hydrochloride) is a metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.

4-Vinylphenol is the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine found in Hedyotis diffusa Willd. 4-Vinylphenol induces apoptosis in vivo.

Phytohemagglutinin (PHA-M) is a lectin, isolated from the red kidney bean , induces apoptosis via increasing proapoptotic protein Bax and activating caspases-3. Anti-tumor activity

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC₅₀ values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

Dorzolamide hydrochloride (MK507 hydrochloride) is the hydrochloride salt form of dorzolamide, an inhibitor of carbonic anhydrase, a zinc-containing enzyme that catalyzes the rapid conversion of carbon dioxide and water into carbonic acid, protons and bicarbonate ions. Distributed throughout many cells and tissues, various carbonic anhydrases play important roles in mineral and metabolic homeostasis.

Sodium Glucoheptonate is used as a kit for Tc-99m radiolabeling, as well as for metal cleaning, mercerizing, paint stripping and aluminum etching. Among other things, Tc-99m glucoheptonate is a kidney and brain imaging agent that can be used to detect brain tumors.

Triglycidyl isocyanurate (Teroxirone) is a triazene triepoxide with antineoplastic and antiangiogenic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. It induces cell apoptosis and can be used for cancer research^[1][2]. Triglycidyl isocyanurate is also used in various polyester powder coatings in the metal finishing industry.