PD-1/PD-L1-IN-25 (compound D2) is an inhibitor of PD-1/PD-L1 interaction with an IC50 value of 16.17 nM. PD-1/PD-L1-IN-25 activates the antitumor immunity of T cells efficiently in PBMCs. PD-1/PD-L1-IN-25 can be used for the research of cancer[1].
(±)-Darifenacin-d4 is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Diacetoxy-6-gingerdiol is a diarylheptanoid isolated from the dichloromethane extract of rhizomes of ginger (Zingiber officinale Roscoe)[1].
Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
Clidinium bromide is an anticholinergic (specifically a muscarinic antagonist) drug, may help symptoms of cramping and abdominal/stomach pain by decreasing stomach acid, and slowing the intestines.
Methyltetrazine-PEG4-maleimide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Cis-trismethoxy resveratrol is a potent anti-mitotic reagent.Cis-trismethoxy resveratrol inhibits tubulin polymerization with an IC50 value of 4 μM[1].
Tyrphostin A51 is a potent protein tyrosine kinase (PTK) inhibitor. Tyrphostin A51 inhibits the volume-dependent release of [3H]taurine in a dose-dependent manner. Tyrphostin A51 markedly reduces cellular tyrosyl phosphorylation level. Tyrphostin A51 inhibits both basal and EGF-induced human bone cell proliferation[1][2].
Tuberculosis inhibitor 8 (compound 3b) is a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative that shows highly active against Mycobacterium tuberculosis (MIC90 of 0.69 μM) and Mycobacterium marinum (MIC90 of 0.69 μM)[1].
Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2)[1].
1,9-Dibromononane-d18 is the deuterium labeled 1,9-Dibromononane[1].
2,3,6-Trimethylphenol-d11 is the deuterium labeled 2,3,6-Trimethylphenol[1].
C87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
N-Nitrosomethylethylamine-d5 is the deuterium labeled N-Nitrosomethylethylamine[1].
A novel potent, selective orally bioavailable MET tyrosine kinase inhibitor with IC50 of <1 nM and 12 nM for unphosphorylated and phosphorylaed MET, respectively; demonstrates potent, broad spectrum activity against MET mutants (V1110I, H1112Y, L1195V, Y1235D, D1228H and M1250T) with IC50 of <1 nM-57 nM, and Y1230 mutants with moderate potency (IC50=25-280 nM); displays >50-fold selectivity in a panel of 130 kinases with exception of Fms and TrkA/B/C; inhibits MET-dependent tumor cell growth in vivo through decreasing phosphorylaed MET.
Tenacissoside I is a C21 steroid from the Marsdenia tenacissima, which is detected at relatively high level in M. tenacissima[1][2].
Atrazine-3-mercaptopropanoic acid is a hapten. The IC50 value of polyclonal antibody (PcAb) 1 with coating Atrazine-3-mercaptopropanoic acid is 7.5 ng/mL[1].
KAT8-IN-1 is a lysine (K) acetyltransferase 8 (KAT8) inhibitor, with IC50s of 141 μM (KAT8), 221 μM (KAT2B), 106 μM (KAT3B), respectively. KAT8 inhibits histone acetyltransferases (HATs), and could result in disease states, such as cancer or inflammatory diseases[1].
Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model[1].
Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
HSGN-218 is an antibacterial agent with low Caco-2 permeability. HSGN-218 efficiently inhibits the growth of different C. difficile species with MIC values ranging from 0.007 μM to 0.07 μM.[1]
Lawsone is a naphthoquinone dye isolated from leaves of Lawsonia inermis that shows antimicrobial and antioxidant activity[1].
Bac2A TFA is an antimicrobial and immunomodulatory peptide. Bac2A TFA is a linear variant of bactenecin and is very effective against fungal pathogens.
Lewis Y tetrasaccharide (Lewis Y, LeY) is a tetrasaccharide derivative form of Lewis X trisaccharide (HY-N10534). Lewis Y tetrasaccharide is an antigen associated with malignant ovarian carcinomas metastasis and poor prognosis[1][2].
Antitumor agent-80 (compound 11) is an orally active and potent antitumor agent. Antitumor agent-80 induces apoptosis in tumor cells[1].
Darbufelone mesylate is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.
Bromochloroacetaldehyde belongs to dihalogenated acetaldehyde and is a byproduct in drinking water. Bromochloroacetaldehyde has genotoxicity[1].
NKH477 (Colforsin dapropate hydrochloride) is a novel water-soluble forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts[1].