ABC34 is an inactive control compound of JJH260. ABC34 does not inhibit the fluorophosphonate reactivity or fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1. ABC34 can inhibit both ABHD6 and PPT122[1].
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor.
VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM).IC50 value: 1 nM (trypsin-like proteasome), 50-100 nM(chymotrypsin-like proteasome), 3 μM (caspase-like proteasome)Target: proteasomein vitro: VR23 is a novel proteasome inhibitor targeting β2 of the 20S proteasome subunit. VR23 produces a synergistic effect in killing multiple myeloma cells, including those that were resistant to bortezomib. VR23 as a structurally novel proteasome inhibitor with desirable properties as an anticancer agent.in vivo: VR23 shows effective antitumor and antiangiogenic activities in mice.
Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor)[1][2][3][4].
Olutasidenib is a highly potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 that could be used in the treatment of acute myeloid leukemia.
EL102 is a inhibitor of HIF1α , Which can inhibit tubulin polymerisation and decreased microtubule stability.target: HIF1αIC 50：20-40 nM.[1]in vitro : EL102 is a cytotoxic agent and also displays cytostatic properties, through flow cytometric analysis of PI-stained cells cultured for 24, 48 and 72?h, following treatment. EL102 induces apoptosis and causes G2/M arrest, preventing the cell from entering into mitosis.In vivo: CWR22 tumours were taken from an in vivo passage, cut into small fragments and transplanted subcutaneously (s.c.) into the flank of 48 nude mice. At day 13, when the tumours were palpable, mice were randomised into 10 groups with 8 mice each and treatment initiated. EL102 12?mg?kg?1 via p.o. (0700 hours and 1700 hours daily).[1]
BPHA is a potent and orally active MMP-2, MMP-9 and MMP-14 inhibitor with 50s of 12 nM, 16 nM and 17 nM, respectively. BPHA does not inhibit MMP-1, -3, and -7 (the IC50s are 974, >1000, and 795 nM, respectively). BPHA has antiangiogenic and antitumor effects[1].
Palmitic acid-d9 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
IDH-305 is an inhibitor of isocitrate dehydrogenase (IDH).
α-Glycosidase-IN-1 (compound MZ7) is a potent α-GLY (α-Glycosidase) inhibitor, with an IC50 of 44.72 nM and a KI of 41.74 nM. α-Glycosidase-IN-1 also shows inhibition profile against human carbonic anhydrase isoenzymes I and II (hCA I and hCA II), and acetylcholinesterase (AChE), with IC50 values of 104.87, 100.04, and 654.87 nM, respectively. α-Glycosidase-IN-1 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy[1].
Rilapladib is a selective Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor with an IC50 of 230 pM.
Mericitabine (R-7128) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator and prevents elongation of RNA transcripts during replication.
D-Tyrosine-d7 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
Doxycycline calcium, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor[1]. Doxycycline calcium shows antibacterial activity and anti-cancer cell proliferation activity[1][2][3][4][5].
LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines[1].
Quinidine polygalacturonate is an antiarrhythmic agent. Quinidine polygalacturonate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine polygalacturonate is also a K+ channel blocker with an IC50 of 19.9 μM, and can induce apoptosis. Quinidine polygalacturonate can be used for malaria research[1][2][3][4].
Enocyanin is an anthocyanin extracted from grapes. Enocyanin shows inhibitory effect on the leucine aminopeptidase, acid phosphatase, γ-glutamyl transpeptidase and esterase activity[1].
4-Ethynyl-L-phenylalanine is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine is a competitive inhibitor with regard to the substrate tryptophan, with a Ki of 32.6 μM. 4-Ethynyl-L-phenylalanine selectively and reversibly inhibits the biosynthesis of serotonin[1].
YCT529 free acid is a potent, selective and orally active RAR-α inhibitor[1].
1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects[1][2].
FXR agonist 5 (compound 1) is a FXR agonist. FXR agonist 5 can be used for research in diseases or disorders caused by metabolic inflammation[1].
Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity. Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation[1].
PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 value of 6.4 µM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia[1].
Moracin P is a 2-arylbenzofuran isolated from the Mori Cortex Radicis. Moracin P exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). Moracin P reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin P has neuroprotective and anti-inflammatory effects[1][2][3].
CCI-006 is a selective inhibitor and chemosensitizer of MLL-rearranged leukemia cells, by inhibits mitochondrial respiration resulting in insurmountable mitochondrial depolarization and a pro-apoptotic unfolded protein response (UPR) in a subset of MLL-r leukemia cells[1].
Arctigenin is a lignan found in certain plants of the Asteraceae; it has shown antiviral and anticancer effects in glass; it is the aglycone of arctiin.IC50 value: Target: anticancer agentArctiin and its aglucone, arctigenin from the fruits of Arctium lappa L. showed potent in vitro antiviral activities against influenza A virus (A/NWS/33, H1N1) (IFV). Based on the data from time-of-addition experiments and on release tests of progeny viruses, arctigenin was assumed to interfere with early event(s) of viral replication after viral penetration into cells, and to suppress the release of progeny viruses from the host cells [1]. arctigenin treatment reduced viability of bladder cancer T24 cells in a dose- and time-dependent manner after treatment with arctigenin (10, 20, 40, 80, and 100 μmol/L) for 24 hr and 48 hr. Arctigenin treatment clearly arrested tumor cells in the G1 phase of the cell cycle. At the molecular level, arctigenin treatment decreased cyclin D1 expression, whereas CDK4 and CDK6 expression levels were unaffected. Moreover, arctigenin selectively altered the phosphorylation of members of the MAPK superfamily, decreasing phosphorylation of ERK1/2 and activated phosphorylation of p38 significantly in a dose-dependent manner [2]. The use of arctigenin has been shown to be effective in a mouse model of Japanese encephalitis [3].
cis-Ferulic acid 4-O-β-D-glucopyranoside (compound 7) is a phenolic glycosid, which can be isolated from Nitraria sibirica.. cis-Ferulic acid 4-O-β-D-glucopyranoside exhibits antioxidant activity and potent inhibitory effect on Phosphatase PTP1B[1].
Finasteride (acetate) is an orally active testosterone 5-alpha-reductase inhibitor. Target: 5-alpha ReductaseApproved: 1992Finasteride (acetate) is the acetate salt of finasteride which is a synthetic 4-azasteroid antiandrogen compound, is a specific inhibitor of steroid Type II 5α-reductase, an intracellular enzyme that converts the androgen testosterone into 5α-dihydrotestosterone (DHT). Finasteride is used in the treatment of prostate cancer, benign prostatic hyperplasia, and androgenetic alopecia (male pattern baldness). In benign prostatic hyperplasia, finasteride inhibits 5alpha-reductase activity in epithelium for Ki of 10nM, significantly lower than in stroma (Ki = 33nM) [1].
Regdanvimab (CT-P59) is a human monoclonal antibody that targets the receptor-binding domain of SARS-CoV-2 spike protein, blocking interaction with ACE2 for viral entry. Regdanvimab can be used for the research of COVID-19[1].