JNJ-6204 is a dual inhibitor for CSNK1D (Casein Kinase 1 Delta) and CSNK1E (Casein Kinase 1 Epsilon) (CSNK1D IC50=2.3 nM; CSNK1E IC50=137 nM). JNJ-6204 shows good brain exposure[1][2].
Pentiapine is a novel dopamine release inhibitor.
Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local anaesthetic. Levobupivacaine exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer[1][2][3].
Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties.
SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC50s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases[1][2].
Myosin Light Chain Kinase Substrate (smooth muscle) is a smooth muscle myosin light chain kinase (MLCK) synthetic peptide substrate[1].
Pentamidine(MP-601205) is an antimicrobial agent.Target: AntiparasiticPentamidine has a potent in vitro antiprotozoal activity. Pentamidine displays cytotoxic activity against L. infantum promastigotes with IC50 of 2.5 μM. 2.5 μM Pentamidine induces early programmed cell death in 49.6% of L. infantum promastigotes. 2.5 μM Pentamidine induces a notorious decrease in promastigotes in both G1 and S phases relative to the control-untreated samples (G1:77.0 vs 15.0%; S:11.0 vs 2.4% for control- and pentamidine-treated promastigotes, resp). Pentamidine is able to bind with calf-thymus DNA (CT-DNA) and induces conformational changes in the DNA double helix. Pentamidine also binds with ubiquitin to modifiy the β-cluster of ubiquitin [1]. Pentamidine is an inhibitor of phosphatase of regenerating liver (PRLs). 1 μg/mL of Pentamidine complete inhibits the activity of recombinant PTP1B in dephosphorylating a phos-photyrosine peptide. 10 μg/mL of Pentamidine completely inhibits the activities of recombinant PRL-1, PRL-2 and PRL-3 in dephosphorylating a phosphotyrosine peptide substrate. Incubation with Pentamidine (1 μg/mL) for 48 h reduces the activity of intracellular PRL phosphatases in transfected NIH3T3 cells by more than 85%. 10 μg/mL Pentamidine completely inhibits the growth of melanoma cell line (WM9), prostate carcinoma cell line (DU145 and C4-2), ovarian carcinoma cell line (Hey), colon carcinoma cell line (WM480), and lung carcinoma cell line (A549) which all express endogenous PRLs [2].
Sitravatinib is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth with IC50 of 3980 nmol/Lin vitro: MGCD516 is superior to other multi-kinase inhibitors in inhibiting cell proliferation, RTK phosphorylation, and phosphorylation of downstream effectors. MGCD516 is unique in a way that it has broad spectrum activity against many RTKs including c-Met, c-Kit, Axl, PDGFR, and Eph receptors that are known to play a role in driving sarcoma cell growthIn vivo: MGCD516 induces significant tumor growth suppression than imatinib and crizotinib.
EtDO-P4 is a nanomolar inhibitor of glycosphingolipid (GSL) synthesis. EtDO-P4 suppresses activation of the EGFR-induced ERK pathway and various receptor tyrosine kinases (RTKs). EtDO-P4 can be used for various types of cancer, including Burkitt’s lymphoma[1].
BigLEN(rat), one of the most abundant peptides in brain, is a potent GPR171 agonist, with an EC50 of 1.6 nM[1][2].
Skp2 inhibitor 2 (14f) is an inhibitor of F-box protein S-phase kinase-associated protein 2 (Skp2), with an IC50 value of 10.2 μM (Skp2-Cks1). Skp2 is a part of cullin-RING ligases, which recruits and ubiquitinates substrates, involving in proteolytic and non-proteolytic process[1].
Quercetin 3,3'-dimethyl ether possesses antioxidant acticity[1].
Aszonalenin is a metabolite of Aspergillus zonatus[1].
JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively[1].
Fmoc-Gly-Pro-Hyp-OH is a tripeptide that can be used in peptide synthesis[1].
Biapenem is a parenteral carbapenem antibacterial agent with a broad spectrum.Target: AntibacterialBiapenem is a carbapenem antibiotic of in vitro antibacterial activity encompassing many Gramnegative and Gram-positive aerobic and anaerobic bacteria, including species producing β-lactamases. Biapenem is more stable than imipenem, mero-penem and panipenem to hydrolysis by human renal dihydropeptidase-I (DHP-I), and therefore does not require the coadministration of a DHP-I inhibitor. In randomised, nonblind or double-blind clinical trials, biapenem showed good clinical and bacteriological efficacy (similar to that of imipenem/ cilastatin) in the treatment of adult patients with intra-abdominal infections, lower respiratory infections or complicated urinary tract infections.
Boc-3-Pal-OH is an alanine derivative[1].
Pomalidomide-PEG4-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in the synthesis of PROTACs..
Avapritinib is a potent and selective exon 17 mutant KIT kinase inhibitor with IC50 of 0.27 nM for KIT D816V.
Notum pectinacetylesterase-1 is a potent inhibitor of notum pectinacetylesterase. Notum pectinacetylesterase-1 can be used for the research of disorders affecting the bone[1].
Perindopril is a long-acting ACE inhibitor of which is used to treat high blood pressure, heart failure or stable coronary artery disease.Target: ACEPerindopril is a long-acting ACE inhibitor. It is used to treat high blood pressure, heart failure or stable coronary artery disease in form of perindopril arginine (trade names include Coversyl, Coversum) or perindopril erbumine (trade name Aceon). According to the Australian government's Pharmaceutical Benefits Scheme website, based on data provided to the Australian Department of Health and Aging by the manufacturer, perindopril arginine and perindopril erbumine are therapeutically equivalent and may be interchanged without differences in clinical effect. However the dose prescribed to achieve the same effect will differ due to different molecular weights for the two forms. Perindopril is one of the most prescribed inhibitors of angiotensin converting enzyme, has a large evidence base, which allows to use it in patients with hypertension, diabetes mellitus type 2, coronary heart disease and chronic heart failure. In this review, the author focused on the evidence of organoprotecting properties of perindopril that lie outside lowering blood pressure.
Microcystin-RR (Cyanoviridin RR) is a potent and orally active protein phosphatase inhibitor. Microcystin-RR induces Apoptosis and ER stress in mice liver[1][2].
Propargyl-PEG2-OH is a PEG-based PROTAC linker can be used in the synthesis of Thalidomide-O-PEG2-propargyl (HY-126458)[1].
Bizelesin (NSC 615291; U-77779) is an AT-specific DNA alkylating agent that can generate DNA interstrand crosslinks, effectively inhibit DNA replication, and has potential anticancer activity[1].
H-D-Phe-Pip-Arg-pNA (S-2238) dihydrochloride, a chromogenic substrate, is patterned after the N-terminal portion of the A alpha chain of fibrinogen, which is the natural substrate of thrombin. H-D-Phe-Pip-Arg-pNA dihydrochloride is specific for thrombin and is used to measure antithrombin-heparin cofactor (AT-III). The AT-III assay using H-D-Phe-Pip-Arg-pNA dihydrochloride is sensitive, accurate, and easy to perform[1][2].
4',7-Dimethoxyisoflavone is isolated from the leaves of Albizzia lebbeck, which shows antifungal activity.
Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker.
MAGE-3 (271-279) is a 271-279 residue peptide derived from melanoma antigens encoded by MAGE-3. MAGE-3 is a cytolytic T lymphocyte (CTL)-defined MAGE-3 protein associated with the human leukocyte antigen (HLA)-A2 molecule. MAGE-3 is overexpressed in different human tumor types, including malignant melanoma, but not by normal tissues except for testis and placenta[1].
Lansoprazole sulfone (AG-1813) is an orally active and selective inhibitor of H+, K+-ATPase. Lansoprazole sulfone can significantly stimulates gastric acid secretion by inhibiting H+, K+-ATPase. Lansoprazole sulfone has potential applications in duodenal ulcer, gastric ulcer, gastroesophageal reflux disease and Zolinger Ellison disease[1][2].
Transcrocetinate disodium, extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.