CB1R Allosteric modulator 5, a novel1-sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonist with an IC50 value of 4.2 μM and EC50 value of ＞10 μM. CB1R Allosteric modulator 5 can be used for the research of metabolic and obesity[1].
PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR, FGFR and Src family activities with nanomolar IC50 values.
hSMG-1 inhibitor 11e is a potent, selective hSMG-1 kinase inhibitor with IC50 of <0.05 nM, >900-fold selectivity over mTOR, and no significant activity against CDK1/2.
Theaflavin 3,3'-digallate (TF3), the typical pigment in black tea, is a good antitumor agent. Theaflavin 3,3'-digallate is generally regarded as the effective component for the inhibitory effects against carcinogenesis without adverse side effects by affecting multiple signal transduction pathways, such as upregulating p53 and p21, inhibiting phosphorylation of the cell survival protein Akt and MAPK pathway, downregulation of NF-κB, shifting the ratio between pro-/antiapoptotic proteins. Theaflavin 3,3'-digallate causes a rapid and sustained decrease in phospho-ERK1/2 and -MEK1/2 protein expression. Theaflavin 3,3'-digallate inhibits HCT116 cell growth with an IC50 of 17.26 μM[1].
Gliadin p31-43 is an undigested gliadin peptide. Gliadin p31-43 induces an innate immune response in the intestine and interferes with endocytic trafficking. Gliadin p31-43 can be used for celiac disease research[1][2].
Yuanhuacine (Gnidilatidin), a daphnane diterpenoid from the flowers of Daphne genkwa with extensive anti-tumor activity. Yuanhuacine is a DNA-damaging agent with orally active[1][2].
Monoethyl phthalate is a phthalate metabolite, acts as a urinary biomarker of phthalates exposure indicating the risks of thyroid cancer and benign nodule[1].
XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50s of 71.1 and 38.1 nM, respectively.
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML[1].
SGK1-IN-2 (14h) is a selective SGK1 (serum and glucocorticoid regulated kinase 1) inhibitor, with an IC50 of 5 nM at 10 μM ATP concentration[1].
4-Hydroxyphenyl Carvedilol is a metabolite of Carvedilol, which is a nonselective beta blocker/alpha-1 blocker.
Cap-dependent endonuclease-IN-3 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-3 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-3 has the potential for the research of influenza A and influenza B infection (extracted from patent WO2019141179A1, compound VI-1)[1].
Lerdelimumab (CAT-152) is an IgG4 human anti-TGF-β2 recombinant monoclonal antibody. Lerdelimumab can be used as an anti-scarring agent for glaucoma research[1][2].
L-NABE is a nitric oxide (NO) synthase inhibitor. L-NABE is also a potent endothelium dependent vasoconstrictor and inhibitor of relaxation[1][2].
Timolol (hemihydrate) is a β-blocker available for both topical and systemic administration. Timolol (hemihydrate) is primarily used to reduce intraocular pressure with open-angle glaucoma and ocular hypertension and Timolol (hemihydrate) also has cardioprotective effect[1][2].
2-Amino-7-cyclopropyl methyl-7,8-dihydro-8-oxo-9-(beta-D-xylo furanosyl)purine (G159-82) PTPD-2 Confidential is a purine nucleoside analogue. 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].
ABH (hydrochloride) is a potent arginase inhibitor. ABH (hydrochloride) can be used for researching anti-inflammation[1].
Cyanine3 DBCO (Cy3-DBCO) hexafluorophosphate is a azide reactive probe, for imaging azide-labeled biomolecules via a copper-free "click-through" reaction.
Glyceryl 1-monooctanoate is a glycerol monolaurate derivative. Glyceryl 1-monooctanoate is a broad-spectrum antimicrobial, suppresses the growth of pathogenic yeast (Candida albicans and Candida parapsilosis), as well as Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli, Klebsiella pneumoniae) bacteria[1].
(Ser(tBu)6,Azagly10)-LHRH is a potent aza-GLY analog[1].
Tyrosinase-IN-11 is a potent tyrosinase inhibitor with IC50s of 50 nM and 64 nM for L-tyrosinase and L-dopa, respectively. Tyrosinase-IN-11 has significant antioxidant activity and low cytotoxicity. Tyrosinase-IN-11 has the potential for skin hyperpigmentation research[1].
Temporin G is an antimicrobial peptide against Legionella pneumophila[1].
Primulic acid II is a saponin isolated from root extract of Primula sp[1].
Isoxazole is a drug scaffold that can be used to develop new drugs with various biological activities (e.g. anti-microbial, anti-viral, anti-cancer, anti-inflammatory, immunomodulatory, anti-convulsant or anti-diabetic properties)[1][2].
Ceftibuten (Sch39720) hydrate, an antibiotic, is an orally active cephalosporin, possesses potent activity in vitro against a wide range of gram-negative and certain gram-positive pathogens[1][2].
Rhodiolin is a flavonoid isolated from Rhodiola fastigita[1].
Verpasep caltespen (HspE7) is a recombinant fusion protein derived from Mycobacterium bovis Calmette-Guérin heat shock protein 65 (Hsp65), the C-terminal end of which is covalently linked to the E7 protein of HPV16. Verpasep caltespen can be used in the study of precancerous and cancerous lesions caused by human papillomavirus (HPV) [1][2].
VO-Ohpic trihydrate is a highly potent inhibitor of PTEN with an IC50 of 46±10 nM.
Cicloxilic acid is a biologically active agent.