Bomedemstat (IMG-7289) ditosylate is an oral and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity[1].
E104 (compound 1) is a potent and selective TLR7 agonist. E104 can be delivered by antibody-drug conjugate (ADC) technology to elicit potent anticancer activity. E104 induces the activation of mouse macrophages and hPBMCs[1].
ICMT-IN-11 (compound 48) is an inhibitor of ICMT (IC50=0.031 μM)[1].
Kapurimycin A3 is an antitumor and antibacterial antibiotic. Kapurimycin A3 has DNA binding and breakage activity. Kapurimycin A3 can be isolated from Streptomyces[1][2].
Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers[1][2].
5’-O-Acetyl-5-acetyloxymethyluridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
Casein kinase 1δ-IN-10 is a casein kinase 1δ (CK1δ) inhibitor (WO2012080729A2; compound 685)[1].
ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells[1].
3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol, a SIRT1 activator, exhibits significant stimulation of SIRT1 activity. Anti-tumor activity[1].
2’-O-Hexadecanyl-2-aminoadenosine is a purine nucleoside analog. 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].
NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively.
GDC-0927 Racemate (SRN-927 Racemate) is a degrader of estrogen receptor, potently inhibits ER-α activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases.
Bromo-PEG1-CH2COOH is a PROTAC linker can be used in the synthesis of PROTACs[1].
Hesperin is a bioactive ingredient present in Japanese horseradish (wasabi) and has been shown to be an Nrf2 activator.
Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model[1].
Quercetin hydrate, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively[1].
Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM). Target: Estrogen Receptor/ERREndoxifen is considered a prodrug, since it has a much higher potency for the estrogen receptor than its parent drug. Endoxifen inhibits the hERG channel protein trafficking to the plasma membrane in a concentration-dependent manner with Endoxifen being more potent than Tamoxifen. [1] Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen observed in Tamoxifen treated patients with deficient CYP2D6 activity (20 to 40 nM) markedly inhibit estrogen-induced cell proliferation rates in the presence of ERβ, whereas much higher Endoxifen concentrations are needed when ERβ is absent.[2]
Pemigatinib is a selective FGFR inhibitor in development for the treatment of patients with cholangiocarcinoma.
Entasobulin is a β-tubulin polymerization inhibitor with potential anticancer activity.
Tricin is a natural flavonoid present in large amounts in rice bran. Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7[1][2][3].
NCT-506 is an orally bioavailable aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with an IC50 of 7 nM[1].
JHU395 is an orally-bioavailable and a plasma stable lipophilic glutamine antagonists (GA) prodrug. JHU395 delivers 6-diazo-5-oxo-L-norleucine (DON) to malignant peripheral nerve sheath tumor (MPNST) in vitro and in vivo, and has antitumor activity in MPNST[1].
N-Boc-PEG9-alcohol is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Ceritinib (LDK378) is a potent and specific ALK inhibitor with an IC50 of 0.2 nM.
DBCO-Sulfo-Link-biotin is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
7-Hydroxychromone is a Src kinase inhibitor with an IC50 of <300 μM.
TLR8 agonist 6 (Compound A) is a TLR8 agonist, with an EC50 of 0.052 μM. TLR8 agonist 6 induces IL-12p40 production in human PBMC (EC50: 0.031 μM). TLR8 agonist 6 can be used in the research of virus resistance, infection resistance, autoimmunity, tumor, etc[1].
Budesonide is a glucocortical steroid with potent anti-inflammatory activity.