F(N-Me)GA(N-Me)IL is a biological active peptide. (Double N-methylated derivatives of amyloidogenic and cytotoxic partial IAPP sequence were found to be devoid of β-sheet structure, amyloidogenicity and cytotoxicity, The derivatives were able to interact with the native sequences and inhibit amyloid formation)
3-Hydroxybakuchiol can be isolated from Otholobium mexicanum J. W. Grimes. 3-Hydroxybakuchiol is an electron transport chain (ETC) inhibitor. 3-Hydroxybakuchiol has antitumor activity, and induces tumor cell apoptosis. 3-Hydroxybakuchiol also has moderate inhibitory activity against α-glucosidase (IC50: 345 μM)[1][2].
Methylophiopogonone B, a homoisoflavonoidal compound that could be isolated from Ophiopogonis Tiber, could scavenge •OH and H2O2 in vitro to a certain extent[1][2].
GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization[1].
NSC16168 is a specific inhibitor of ERCC1-XPF, with an IC50 value of 0.42 μM. NSC16168 inhibits DNA repair and potentiates CDDP efficacy in cancer[1].
Ethyl 3-coumarincarboxylate is a coumarin derivative. Ethyl 3-coumarincarboxylate can be used as a pseudo-template to give a molecularly imprinted polymer (MIP) that has a fairly specific recognition capability for aflatoxins[1].
3',5'-Bis-O-benzoyl-2'-deoxy-2'-fluoro-4-deoxy-arabinouridine 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].
Neuropeptide Y5 receptor ligand-1 (compound 54), a carbazole derivative, is a potent neuropeptide Y5 (NPY-5) receptor antagonist[1].
Tertiapin-Q is a highly selective blocker of GIRK1/4 heterodimer and ROMK1 (Kir1.1).
mAChR antagonist 1 (compound 4a) is a mAChR antagonist with Ki values of 255 nM, 121 nM, 158 nM, and 255 nM for M1, M3, M4, and M5 subtype, respectively[1].
Thymocartin (Thymopoietin II (32-35)) is the 32-35 fragment of the thymic factor (thymopoietin). Thymocartin has shown potential for immunodeficiency diseases research[1][2].
Zoptarelin doxorubicin (AEZS-108; AN-152) is a hybrid anticancer agent, containing Zoptarelin and Doxorubicin. Zoptarelin doxorubicin has been used to research targeting tumors expressing LHRH receptors. Zoptarelin doxorubicin abolishes tumor progression and induces remarkable apoptosis in vitro[1].
Curvulinic acid is a phytotoxic compound, has herbicidal activity[1].
Fludarabine (phosphate) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.
Bentazone is a post-emergence herbicide used for selective control of broadleaf weeds and sedges in beans, rice, corn, peanuts, mint and others. It acts by interfering with photosynthesis[1].
Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene[1]. Lapaquistat acetate (TAK-475) is originally intended use to Mevalonate Kinase Deficiency (MKD), it is effective at lowering low-density lipoprotein cholesterol, but it might cause liver damage[2].
Lecithin is regarded as a safe, conventional phospholipid source. Phospholipids are reported to alter the fatty acid composition and microstructure of the membranes in animal cells.
Regaloside D is a phenylpropanoid isolated from Lilium Longiflorum[1].
cp028 is a potent pre-mRNA splicing inhibitor. cp028 inhibits splicing in HeLa nuclear extract with an IC50 value of 54 µM[1].
PCSK9 degrader 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) degrader. PCSK9 degrader 1 does not affect PCSK9 function[1].
CRT, an iron peptide mimic, can bind to apo-transferrin (apo-Tf). CRT can be used to modify nanoparticles, and enhances drug delivery efficiency[1].
cis,cis-Muconic acid, a metabolic intermediate of Klebsiella pneumonia, can be converted to adipic acid and terephthalic acid, which are important monomers of synthetic polymers. cis,cis-Muconic acid is also a biochemical material that can be used for the production of various plastics and polymers and is particularly gaining attention as an adipic acid precursor for the synthesis of nylon-6,6[1][2].
Sideroxylonal A is an effective marine antifouling agent isolated from Eucalyptus jensenii. Sideroxylonal A has antibacterial activity against the Gram-positive bacteria Staphylococcus aureus and Bacilus subtilis[1].
Pimroctakin (bovine) is a IL-8 analogue[1].
CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy[1].
Clodronic acid (Clodronate) disodium salt, a first-generation bisphosphonate, is orally active osteoclastic bone resorption inhibitor. Clodronic acid disodium salt can be used in high bone turnover states, Paget’s disease and osteolytic bone metastases[1][2][3].
Docusate Sodium is a laxative used to treat constipation, for constipation due to the use of opiates it maybe used with a stimulant laxative, can be taken by mouth or rectally.
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis[1][2].
SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5 > 300 μM), and is more potent than Resveratrol and the closest sirtuin homologues[1].
Lenalidomide-5-Br is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-Br can be connected to the ligand for protein by a linker to form PROTAC[1].