antigen-1

MART-1 nonamer antigen (LAGIGILTV) is a melanoma antigen recognizable by T cells. It functions as a superagonist by enhancing the immunological response of specific T cells when induced ex vivo. Additionally, MART-1 nonamer antigen serves as a peptide model for designing antitumor vaccines.

Mage-1 Antigen (161-169), human is a polypeptide molecule with the sequence EADPTGHSY.

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6 20 22 nM for Raf-1 VEGFR-3 B-Raf).

Lifitegrast (SAR 1118) is an antagonist of lymphocyte function-associated antigen-1.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

NCGC00262650 is an inhibitor of AMA1-RON2 interaction and c-Src tyrosine kinase activity.

RWJ 50271 is a selective lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction inhibitor( IC50 of 5.0 μM in HL60 cells).

Asoxime dichloride (Tert-Butyl2-(2-hydroxyethyl)-1-pyrrolidinecarboxylate) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system. Asoxime dichloride involves in modulating immunity response.

BI-1950 is a highly potent inhibitor of lymphocyte function-associated antigen-1 (LFA-1), an essential component in normal immune system function and a significant target for drug discovery [1].

BMS-688521 BMS-688521 is an orally active and potent inhibitor of LFA-1 ICAM interaction, a small molecule antagonist of leukocyte function-associated antigen-1 (LFA-1), with potential anti-inflammatory activity.

m-PEG4-Br is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADC) for Trastuzumab, positioned distally from the monomethyl auristatin E (MMAE) payload to produce an ADC with modified hydrophilicity, antigen binding, and in vitro potency[1].

CQ-16 is an orally active small molecule drug conjugate (SMDC) that targets prostate-specific membrane antigen (PSMA). It exhibits high selectivity in its antiproliferative activity between PSMA-positive and PSMA-negative prostate cells. Additionally, CQ-16 possesses PARP inhibitory activity (IC50=1 nM).

CBX-12 is a peptide drug conjugate (PDC) that targets tumors in an antigen-independent manner and exhibits antitumor activity. Comprising a pH-sensitive peptide (pHLIP), an auto-cleavable linker, and the topoisomerase 1 (TOP1) inhibitor Exatecan, it effectively targets cancerous cells.

SKLB4771 (FLT3-IN-1) is a novel potent and selective Flt3 inhibitor.

STF-1084 is an inhibitor that cannot penetrate cells and targets ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (ENPP1) with an apparent Ki of 0.11 µM. It demonstrates selectivity for ENPP1 over ENPP2 and alkaline phosphatase (ALP) with apparent Kis of 5.5 and >100 µM, respectively, and does not affect a panel of 468 kinases at 1 µM. STF-1084 hinders the extracellular breakdown of cGAMP in ENPP1-overexpressing and cGAS-expressing 293T cells, with an IC50 of 0.340 µM, and enhances mRNA expression for the gene encoding IFN-β in CD14+ primary human peripheral blood mononuclear cells (PBMCs) when incubated with conditioned medium from ENPP1-overexpressing and cGAS-expressing 293T cells treated with STF-1084. In a live setting, STF-1084, when combined with ionizing radiation, elevates the proportion of tumor-associated CD11c+ cells among antigen-presenting cells (APCs) in a murine mammary cancer model (4T1).

A 286982 is an inhibitor that blocks the integrin-ligand interaction between leukocyte function-associated antigen-1 (LFA-1) and intercellular adhesion molecule-1.

TC-SP 14, also known as compound 14, is a highly active and potent S1P1 agonist with oral bioavailability. It exhibits an EC50 value of 0.042 μM, indicating its strong binding affinity to the S1P1 receptor. Notably, its interaction with the S1P3 receptor is minimal, as evidenced by an EC50 value of 3.47 μM. TC-SP 14 demonstrates significant pharmacological effects, including a marked reduction in blood lymphocyte counts and the attenuation of delayed type hypersensitivity response to antigen challenge [1].

CDP-840 (GR259653X) is a potent, selective, and orally active phosphodiesterase IV (PDE IV) inhibitor that specifically inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys [1].

APC 366 is a selective tryptase inhibitor (Ki = 7.1 μM). Tryptase is a serine protease released during mast cell degranulation, which reduces acute airway responses to allergens and can be used for asthma allergy treatment.

Linifanib (AL-39324) (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).

HUHS015 is a potent PCA-1 ALKBH3 inhibitor.

T2AA (4-[4-[(2S)-2-amino-3-hydroxypropyl]-2,6-diiodophenoxy]phenol) is an inhibitor of proliferating cell nuclear antigen (PCNA) with IC50 of 1 μM for PCNA PIP-box peptide interaction. T2AA suppresses cancer cell growth and causes DNA replication stress by stalling DNA replication forks and inhibiting PCNA interaction with DNA polymerase δ.

Destruxin B2 is a cyclic hexadepsipeptide mycotoxin that has been found in M. anisopliae and has antiviral, insecticidal, and phytotoxic activities.1,2,3 It inhibits secretion of hepatitis B virus surface antigen (HBsAg) by Hep3B cells expressing hepatitis B virus (HBV) DNA (IC50 = 1.3 μM).1 Destruxin B2 is toxic to Sf9 insect cells in an electric cell-substrate impedance sensing (ECIS) test with a 50% inhibitory concentration (ECIS50) value of 92 μM.4 It is also phytotoxic to B. napus leaves.3 |1. Yeh, S.F., Pan, W., Ong, G.-T., et al. Study of structure-activity correlation in destruxins, a class of cyclodepsipeptides possessing suppressive effect on the generation of hepatitis B virus surface antigen in human hepatoma cells. Biochem. Biophys. Res. Commun. 229(1), 65-72 (1996).|2. Male, K.B., Tzeng, Y.-M., Montes, J., et al. Probing inhibitory effects of destruxins from Metarhizium anisopliae using insect cell based impedance spectroscopy: Inhibition vs chemical structure. Analyst 134(7), 1447-1452 (2009).|3. Buchwaldt, L., and Green, H. Phytotoxicity of destruxin B and its possible role in the pathogenesis of Alternaria brassicae. Plant Pathol. 41(1), 55-63 (1992).