h-NTPDase-IN-5 (compound 3b) is a pan-inhibitor of NTPDase with IC50s of 1.10 μM (h-NTPDase1), 44.73 μM (h-NTPDase2), 26.14 μM (h-NTPDase3), 0.32 μM (h- NTPDase8).
CPI-1205, a highly potent and selective EZH2 inhibitor (biochemical IC50=2 nM, cellular EC50=32 nM).
Azido-PEG4-alpha-D-mannose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(Tyr0)-C-Peptide (dog) is a peptide[1].
ARG1-IN-1 is a human arginase 1 inhibitor with an IC50 of 29 nM.
Dodecyl L-alaninate hydrochloride is an alanine derivative[1].
CCT245737 is a orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM。
4-Nonylphenol polyethoxylate is an organic compound that is a nonionic surfactant; widely used in contraceptives for its spermicidal properties.
Sulfadimethoxypyrimidine D4 is a deuterium labeled Sulfadimethoxypyrimidine. Sulfadimethoxypyrimidine is a sulfonamide antibiotic with a broad-spectrum antibacterial effect[1].
Ginkgetin is a natural biflavonoid isolated from leaves of Ginkgo biloba L; effects of anti-inflammation and anticancer have been reported.IC50 value:Target:in vitro: Ginkgetin inhibits COX-2 dependent phases of prostaglandin D(2) (PGD(2)) generation in bone marrow-derived mast cells (BMMC) in a concentration-dependent manner with IC(50) values of 0.75 microM. Ginkgetin consistently inhibited the production of leukotriene C(4) (LTC(4)) in a dose dependent manner, with an IC(50) value of 0.33 microM. Ginkgetin also inhibited degranulation reaction in a dose dependent manner, with an IC(50) value of 6.52 microM [1]. Ginkgetin inhibited both inducible and constitutively activated STAT3 and blocked the nuclear translocation of p-STAT3 in DU-145 prostate cancer cells. Furthermore, ginkgetin selectively inhibited the growth of prostate tumor cells stimulated with activated STAT3. Ginkgetin induced STAT3 dephosphorylation at Try705 and inhibited its localization to the nucleus, leading to the inhibition of expression of STAT3 target genes such as cell survival-related genes (cyclin D1 and survivin) and anti-apoptotic proteins (Bcl-2 and Bcl-xL) [2]. Ginkgetin suppressed the viability of PC-3 cells in a concentration-dependent manner and also significantly increased the sub-G1 DNA contents of cell cycle in PC-3 cells. Ginkgetin activated caspase-3 and attenuated the expression of survival genes such as Bcl-2, Bcl-xL, survivin and Cyclin D1 at protein and mRNA levels [3]. Ginkgetin (1 - 10 microM) and the biflavonoid mixture (10 - 50 microg/ml), mainly a 1 : 1 mixture of ginkgetin and isoginkgetin, from G. biloba leaves, inhibited production of prostaglandin E2 from lipopolysaccharide-induced RAW 264.7 cells [4].in vivo: Ginkgetin inhibited tumor growth in xenografted nude mice and down-regulated p-STAT3Tyr705 and survivin in tumor tissues [2]. At total doses of 1,000 microg/site on the dorsal skin (15 mm x 15 mm), ginkgetin inhibited prostaglandin E2 production by 65.6 % along with a marked suppression of COX-2 induction. In addition, ginkgetin and the biflavonoid mixture (100 - 1,000 microg/ear) dose-dependently inhibited skin inflammation of croton oil induced ear edema in mice by topical application [4].
(±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Ziprasidone (CP-88059) mesylate is an orally active combined 5-HT and dopamine receptor antagonist[1]. Ziprasidone mesylate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM)[1].
18-Nor-abieta-8,11,13-triene-4,15-diol (Compound 20) is a natural product that can be isolated from Abies georgei[1].
Taurox SB can be used as a nontoxic, non-antimicrobial agent that can replace or supplement the use of antibiotics in the animal husbandry of livestock animals to increase health and general well-being, productivity, feed efficiency and weight gain.
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(d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin (d(CH2)5[Tyr(Me)2, Dab5]AVP) is a specific antagonist of vasopressin V1a receptor, with a pA2 of 6.71[1].
Batatasin III, a stilbenoid, inhibits cancer migration and invasion by suppressing epithelial to mesenchymal transition (EMT) and FAK-AKT Signals. Batatasin III has anti-cancer activities[1].
8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50Epac and is a potent Epac activator[1][2].
HIV-1 inhibitor-19 is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-19 maintains its inhibitory activity against L100I, K103N and V106A/ F227L mutant strains with EC50s of 7.3 nM, 9.2 nM and 21.0 nM, respectively[1].
O-Acetylschisantherin L (Acetylschisantherin L) is a natural lignan, which exhibits inhibitory effects on LPS-induced NO production in BV-2 cells with an IC50 of 23.1 μM[1].
Amentoflavone 7,4',7'',4'''-tetramethyl ether, a biflavone, is a natural product that can be isolated from Selaginella moellendorffii[1].
(R)-2-Amino-2-(tetrahydro-2H-pyran-4-yl)acetic acid is a Glycine (HY-Y0966) derivative[1].
1-Oxo-4-hydroxy-2-en-4-ethylcyclohexa-5,8-olide (compound 8) is a potent anti-ulcer agent[1].
Boc-β-HoArg(Tos)-OH is an arginine derivative[1].
BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research[1].
(R)-TAPI-2 is the isomer of TAPI-2 (HY-100211A). TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP[1]. TAPI-2 blocks the entry of infectious SARS-CoV[2].
Chloroquine (diphosphate) is an antimalarial and anti-inflammatory drug widely used to treat malaria and rheumatoid arthritis. Chloroquine is an inhibitor of autophagy and toll-like receptors (TLRs).
Sodium diethylglycinate is a Glycine (HY-Y0966) derivative[1].
GSK1521498 is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs[1].