Rolistobart is a humanized immunoglobulin G4-kappa, anti-LILRB4/CD85k monoclonal antibody. Rolistobart is an immunostimulant and antineoplastic[1].
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition[1][2].
[Arg15,20,21, Leu17] VIP-Gly-Lys-Arg-NH2 is a vasoactive intestinal polypeptide (VIP) analog with relaxant effects[1].
2-(Pyridin-2-yl)acetic acid-d2 (hydrochloride) is the deuterium labeled 2-(Pyridin-2-yl)acetic acid hydrochloride[1].
Xanthalin (compound 2) is a characteristic component isolated from Peucedanum ledebourielloides root[1].
NaPi2b-IN-2 (compound 5) is a potent inhibitor of sodium-dependent transport protein 2b (SLC34A2, NaPi2b), with an IC50 of 38 nM for human NaPi2b. NaPi2b-IN-2 can be used for the research of hyperphosphatemia[1].
Tricosane-d48 is the deuterium labeled Tricosane[1].
Vitexin B-1 is an inhibitor of Bcl-2 and the agonist of Caspase. Vitexin B-1 has cytotoxic effect and induces apoptosis in MCF-7, ZR-75-1, MDA-MB-231, and COC1 cells with IC50s of 3.2, 2.1, 1.8 and 0.39 μM, respectively[1].
Pegacaristim is a monoclonal antibody with thrombopoietic activity. Pegacaristim can promote generation of platelets[1][2].
Sternbin is the detoxified metabolites from the rice flavanone phytoalexin Sakuranetin by Pyricularia oryzae. Sakuranetin is a flavanone phytoalexin associated with disease resistance in rice plants[1].
TSHR antagonist S37 is a selective and competitive thyrotropin receptor (TSHR) antagonist. TSHR antagonist S37 is the racemate of TSHR antagonist S37a[1].
Anthriscinol is a natural product that can be isolated from Anthriscus sylvestris HOFFM[1].
Sodium caseinates, the salt of casein, are the main milk protein. Sodium caseinate are able to induce proliferation and activation of granulocytes as well as increase the serum concentration of two key cytokines, GM-CSF and G-CSF. Sodium caseinate induces mouse granulopoiesis[1].
α-Hemolysin (Staphylococcus aureus) is one of the most characteristic virulence factors secreted by Staphylococcus aureus, a polypeptide capable of destroying the host cell plasma membrane. After α-Hemolysin binds to the cell surface, its monomers assemble into a homoheptamer to form a front pore, which then transforms into a mature transmembrane pore water channel, allowing K+ and Ca2+ ion transport, leading to necrotic death of target cells[1].
Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz inhibits human placenta microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an antagonist of the estrogen receptor (ER) and androgen receptor (AR) (IC50s = 25 μM and 4 μM, respectively) as well as activates the aryl hydrocarbon receptor (AhR; EC50 = 1 μM).
(E/Z)-Mycophenolic Acid-13C,d3 is the deuterium and 13C labeled (E/Z)-Mycophenolic Acid[1].
NS19504 is a Ca2+-activated K+ channel (BK channel, KCa1.1 channel) activator (EC50=11.0 µM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions[1].
2-Amino-3-(2-fluorophenyl)propanoic acid is a phenylalanine derivative[1].
XIAP antagonist 1 (compound A4) is a XIAP-specific antagonist, XIAP antagonist 1 degradation of XIAP via the ubiquitin-proteasome pathway[1].
8-Methyladenosine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Folinic acid (Leucovorin) calcium hydrate is a biological folic acid and is generally administered along with Methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity[1].
XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), but XY1 is completely inactive.Target: PRMT3XY1 is a close analogue of SGC707, is completely inactive againstPRMT3 at concentrations as high as 100 μM. XY1 contains a naphthyl group replacing the isoquinoline group, lacks the key hydrogen bond with T466. The naphthyl ring of XY1 could act as a weak hydrogen-bond acceptor, but this should come with a substantial enthalpic penalty. The more than 1000-fold potency loss of XY1 compared with SGC707 supports this analysis. It is unclear whether other factors such as electronic effects also contributed to the potency loss of XY1 compared with SGC707. SGC707 and XY1 are a pair of excellent tools for the biomedical community to further elucidate biological functions and disease associations of PRMT3.
AP102 is a dual SSTR2/SSTR5-specific somatostatin analog (SSA). AP102 is a disulfide-bridged octapeptide SSA containing synthetic iodinated amino acids. AP102 binds with subnanomolar affinity to SSTR2 and SSTR5 (IC50: 0.63 and 0.65 nM, respectively). AP102 does not bind to SSTR1 or SSTR3. AP102 can be used for acromegaly and neuroendocrine tumors research[1].
Amine-PEG4-amido-tri-(carboxyethoxymethyl)-methane is a organic compounds, acts as a linker used to synthesize multifunctional molecules.
SW106065 is an apoptosis inducer in malignant peripheral nerve sheath tumors (MPNST). SW106065 inhibits ATP consumption of sMPNST and other models of MPNST with an EC50 of 1 µM. SW106065 can be used for MPNST research[1].
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor[1].
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity[1].
Ac-Leu-Arg-AMC is a fluorogenic peptide substrate.
Thrombospondin-1 (1016-1021) (human, bovine, mouse), a Thrombospondin-1-derived peptide, is a truncated peptide devoid of CD47-binding activity[1].
Tetrazine-biotin is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].