MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM[1].
Tavolixizumab (MEDI 0562; Tavolimab) is a human monoclonal antibody to TNFRSF4 (TNF receptor superfamily member 4) for use in cancer immunology research[1].
Amifostine is a broad-spectrum cytoprotection agent against the DNA damaging effects of ionizing radiation and chemotherapy drug.
Calyculin A is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC50s of 0.5 to 1 nM.
AP 24149 is a potent Src-Abl dual inhibitor with IC50 values of 9.1, 3.6 nM for Src and Abl, respectively[1].
TP-064 is a potent, selective, and cell-active inhibitor of PRMT4 with IC50 of <10 nM and Kd of 7.1 nM, shows high selectivity (>100-fold) for PRMT4 over other PRMTs; reduces dimethylation of BAF155 (IC50=340±30 nM) and MED12 (IC50=43±10 nM) in a dose-dependent manner in cell-baed assays; inhibits the proliferation of a subset of multiple myeloma cell lines (NCI-H929, RPMI8226, Cell IC50 of 379 and 886 nM, respectively) with affected cells arrested in G1 phase of the cell cycle, but has no effect on acute myeloid leukemia, colon cancer, or lung cancer cell lines.
Gemtuzumab (Gemtuzumab ozogamicin) is an antibody-drug conjugate (ADC) consisting of a monoclonal antibody targeting CD33 linked to a cytotoxic derivative of Calicheamicin. Gemtuzumab can be used for the research of acute myeloid leukemia[1].
BET-IN-2 is a BET inhibitor with an IC50 of 52 nM for BRD4-BD1.
INT-767 is a dual farnesoid X receptor/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively.
Thalidomide-5-propoxyethanamine is the Thalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein[1].
(S)-Monastrol ((+)-Monastrol) is an allosteric inhibitor of the mitotic kinesin Eg5 that exhibits an antiproliferative effect against several cancer cell lines. (S)-Monastrol arrests mammalian cells in mitosis with monopolar spindles[1][2].
ND1-YL2 is a PROTAC that selectively degrades SRC-1 via the N-degron pathway. ND1-YL2 significantly inhibits cancer invasion and migration in vitro and in vivo. ND1-YL2 can be used in cancer research[1].
MAT2A inhibitor is a methionine adenosyltransferase 2A (MATA2 ) inhibitor extracted from patent US20180079753, compound example 196 (4).
The compound 19 (QW30) shows potent antitumor activity with an IC50 value of 0.33 μM.
Pexidartinib (PLX-3397) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13 nM, 27 nM, and 11 nM for CSF1R, c-Kit, and FLT3, respectively.
A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.In vitro: A-804598 potently blocked IL-1β release in the THP-1 cells (IC50 of 8.5 nM). A-804598 also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50 of 8.1 nM) with similar potency as in the calcium-influx assay. [1]In vivo: Autoradiographic analysis of coronal rat brain sections revealed that there was specific binding of [3H]-A-804598 throughout the rat brain. High levels of [3H]-A-804598 specific binding were also found in the grey matter of the L4-L6 region of the rat spinal cord. [2]
L-Serine-13C3,15N ((-)-Serine-13C3,15N) is the 13C- and 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
PRMT5-IN-18 (Compound 002) is a potent PRMT5 inhibitor that can be used for the research of a disease mediated by PRMT5， such as cancer[1].
MK-8745 is an aurora A kinase inhibitor with IC50s of 0.6 nM.
AZ876 is a novel high-affinity LXR agonist. AZ876 was 25-fold and 2.5-fold more potent than GW3965 (HY-10627) on human (h)LXRα and hLXRβ respectively.(1) AZ876 suppressed up-regulation of hypertrophy- and fibrosis-related genes, and further inhibited prohypertrophic and profibrotic transforming growth factor β (TGFβ)-Smad2/3 signalling.(2) AZ876 prevented TGFβ- and angiotensin II-induced fibroblast collagen synthesis, and inhibited up-regulation of the myofibroblastic marker, α-smooth muscle actin.(3) The reference for administration is 20 umol/kg/day in vivo.
(Rac)-CPI-203 is a racemate of CPI-203 (HY-15846) (BET bromodomain inhibitor)[1]
Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-2 3CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis[1][2][3].
Alkannin, found in Alkanna tinctoria, is used as a food coloring. Alkannin shows anticancer activity, arrests cell cycle, and induces apoptosis. Alkannin improves hepatic inflammation in a Rho-kinase pathway[1][2][3].
m-PEG11-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Acyclovir (Aciclovir) sodium is a potent, orally active antiviral agent. Acyclovir sodium has antiherpetic activity with IC50 values of 0.85 μM and 0.86 μM for HSV-1 and HSV-2, respectively. Acyclovir sodium induces cell cycle perturbation and apoptosis. Acyclovir sodium prevents bacterial infections during induction therapy for acute leukaemia[1][2][3][4].
Antitumor agent-44 (Compound 5n) disrupts the mitochondrial homeostasis, induces cell cycle arrest and apoptosis in human adenocarcinoma cells. Antitumor agent-44 (Compound 5n) possesses good anti-tumor activity in a lung-cancer-cell xenograft mice model[1].
CIA-1 inhibits the nuclear receptor COUP-TFII, with IC50s ranging from 1.2 μM to 7.6 μM in prostate cancer cell lines.CIA-1 inhibits the growth of a variety of prostate cancer cell lines in vitro and inhibits COUP-TFII activity to regulate its target genes.CIA-1 in vivo exhibits tumor growth inhibitory effects in a mouse model of prostate cancer xenografts. inhibitory effect on tumor growth in a xenograft mouse model of prostate cancer in vivo.
E3 ligase Ligand 15 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 15 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].
PSB-0788 (compound 17), xanthine-8-yl-benzenesulfonamide derivative, is a new selective high-affinity A2B antagonist with IC50 value of 3.64 nM and Ki value of 0.393 nM, respeactively. PSB-0788 (compound 17) can be used for the research for chronic inflammatory lung diseases[1].
Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic[1][2].