Plantarenaloside is an iridoid glucoside that can be isolated from Leucocarpus perfoliatus G. DON[1].
Drospirenone-d4 (Dihydrospirorenone-d4) is the deuterium labeled Drospirenone. Drospirenone (Dihydrospirorenone) is a synthetic progestin that is an analog to spironolactone[1][2].
Seneciphylline N-Oxide is a dehydrogenation product of Senecionine N-oxide. Seneciphylline N-Oxide is a natural compound isolated from root cultures of Senecio erucifolius (Asteraceae)[1].
1,1,1,1-Kestohexaose is a fructan oligomer isolated from Poa ampla[1].
PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM.
GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity[1].
AY 9944 is a specific cholesterol biosynthesis inhibitor. AY 9944 inhibits the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50=13 nM). AY 9944 causes hypocholesterolemia and accumulation of 7DHC. At high doses, AY 9944 inhibits also in cultured embryos sterol Δ7-Δ8 isomerase, which causes the accumulation of cholest-8-en-3β-ol[1][2][3].
(+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease[1][2].
JNJ-26489112 (JNJ26489112) is a broad-spectrum anticonvulsant that displays activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures; exhibits very weak inhibition of human CA-II (IC50=35 μM); inhibits Na+, kainate, and KCNQ2 channels to varying degrees, while moderately potentiating GABA current and inhibiting N-methyl-D-aspartic acid current, its action at several targets appears to be responsible for the observed neurostabilizing effects; shows limited seizure spread and elevated seizure threshold in preclinical animal models. Epilepsy Discontinued
Hikizimycin is a potent anthelmintic and antibacterial natural product.
Aristolan-1(10)-en-9-ol is a sesquiterpene that can be isolated from Laurencia similis[1].
2,4′-Dichloroacetanilide is a fungistatic agent. 2,4′-Dichloroacetanilide inhibits T. asteroides with a MIC value of 6.25 μg/mL[1].
LUF7346 is a novel hERG allosteric modulator that slows IKr deactivation and positively shifting IKr inactivation; rescues the genetic form of LQTS, reverses drug-induced LQTS and correct thes combination of genetic and drug-induced LQTS; normalises both action- and field potentials (AP and FP, respectively) in all hPSC-CMs by slowing IKr deactivation and positively shifting the IKr inactivation.
Thalidomide-Piperazine-Piperidine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
OBAA is a potent phospholipase A2 (PLA2) inhibitor with an IC50 of 70 nM. OBAA blocks Melittin-induced Ca2+ influx in Trypanosoma brucei with an IC50 of 0.4 μM[1][2][3].
N-(m-PEG4)-N'-(azide-PEG4)-Cy3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Isorhapontigenin, an orally bioavailable dietary polyphenol isolated from the Chinese herb Gnetum cleistostachyum, displays anti-inflammatory effects. Isorhapontigenin induces autophagy and inhibits invasive bladder cancer formation[1][2].
Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor. Pimonidazole is used for intravenous administration followed by biopsy, it can be used for qualitative and quantitative assessment of tumor hypoxia[1].Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group[2].
Neuromedin U-8 (porcine) is a biologically active peptide.
Uvarigranol B, a polyoxygenated cyclohexene, is obtained from the roots of Uvaria grandiflora Roxb (Annonaceae)[1].
Kaempferol 3,7-bis(α-L-rhamnose-D-glucose) (compound 1) is a flavonoid glycoside that can be found in Euonymus fortune.
Pomalidomide-PEG6-butyl iodide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 6-unit PEG linker used in PROTAC technology[1].
Tubulin polymerization-IN-30 (compound 6e) is a potent Tubulin polymerization inhibitor. Tubulin polymerization-IN-30 is a colchicine binding site inhibitor. Tubulin polymerization-IN-30 can disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. Tubulin polymerization-IN-30 exhibits the high potency against the cancer cell lines including SGC-7901, A549 and HeLa, with IC50 values of 2.16, 2.21, and 0.403 μM[1].
Denudaquinol is a phenolic derivative. Denudaquinol can be isolated from M. denudata. Denudaquinol has cytotoxicity against the SFME and r/mHMSFME-1 cell lines[1].
2',3'-O-Isopropylidene-5-pyrrolidinomethyl-2-thiouridine 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].
N2S2-CBMBC, an N2S2 bromo-benzyl ether derivative, acts as a ligand and use 99mTc-labelled complexes 99mTc-N2S2-CBMBC can be used as an imaging agent to be applied to the aspect of detecting PD-L1 expression, realize the real-time, comprehensive and convenient detection of the PD-L1 level of tumors, and overcome the defects of an immunohistochemical method[1].
Siamenoside I is one of the mogrosides that has several kinds of bioactivities.
UKI-1 is a novel synthetic inhibitor of the urokinase-type plasminogen activator system. It can also inhibits the invasive capacity of carcinoma cells. (Ki=0.41 μM)In vitro : A decrease of tumor cell invasion by up to 50% was achieved in both models with the SCCHN line FaDu and the cervical carcinoma line HeLa after treatment with UK1.
ODN M362, a class C oligodeoxynucleotide, is a TLR-9 agonist and can be used as a vaccine adjuvant. ODN M362 induces cancer cell apoptosis[1][2].
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1[1].