NSC689857 is a potent EGFR and SCFSKP2 inhibitor with an IC50 value of 36 μM for Skp2-Cks1. NSC689857 can inhibit p27 ubiquitylation (IC50=30 μM). NSC689857 has varied activity across cancer types, with more activity against leukemia cell lines than others[1][2].
HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer[1].
Deltarasin hydrochloride is an inhibitor of KRAS-PDEδinteraction with Kd of 38 nM for binding to purified PDEδ.
Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM[1]. Antianemia agent[1].
ML299 is a potent, CNS penetrant, dual phospholipase PLD1/PLD2 probe with IC50 of 6 nM/20 nM, respectively; robustly increases caspase 3/7 activation under serum-free conditions, provides a dose-dependent decrease (100 nM to 10 uM) in invasive migration in U87-MG cells, with statistical significance reached at both the 1 uM and 10 uM doses.
Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential use in the treatment of Alzheimer's disease (AD).
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans[1][2][3].
Mitochonic acid 5 binds mitochondria and ameliorates renal tubular and cardiac myocyte damage. Mitochonic acid 5 modulates mitochondrial ATP synthesis.
Fluvastatin (Leschol) inhibits HMG-CoA reductase activity with IC50 of 8 nM.IC50 value: 8 nMTarget: HMG-CoA reductaseFluvastatin is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Human hepatocellular carcinoma cell (HCC) studies indicate that Fluvastatin induces G2/M phase arrest. In the presence of Fluvastatin, HCC cells show a decrease of Bcl-2 and procaspase-9 expression, and an increase in Bax, cleaved caspase-3, and cytochrome c. Fluvastatin is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.
CM10 is a potent and selective aldehyde dehydrogenase 1A family inhibitor (ALDH1Ai), with IC50s of 1700, 740, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. CM10 does not inhibit any of the other ALDH family members. CM10 can regulate metabolism and has anti-cancer activity[1].
HA130 is a selective ATX (autotaxin) inhibitor with IC50 of 28 nM. IC50 value: 28 nM [2]Target: ATXin vitro: HA130 completely blocks the ability of ATX to promote TEM (transendothelial migration). HA130 at 0.3 μM completely ablates the activity of ATX on TK1 uropod formation. [1]in vivo: HA130 instantaneously lowers plasma levels of LPA in mice after intravenous administration. HA130 is an inhibitor of the enzymatic activity of ATX, slows T cell migration across lymph node HEVs. HA130 decreased the "outside HEVs/inside HEVs" ratio by 3-4-fold, compared to vehicle-treated animals vehicle (p < 0.01 for both PLNs and MLNs). [1]
Vibsanin A, a protein kinase C (PKC) activator, exhibits anti-proliferative activity against human cancer cell lines. Vibsanin A is also a HSP90 inhibitor[1].
Enpp-1-IN-2 (Compound C) is a potent ENPP1 (ectonucleotide pyrophosphatase/phosphodiesterase 1) inhibitor with IC50 values of 0.26, 0.48 and 2.0 μM evaluated by means of TG-mAMP, pNP-TMP, and ATP assays, respectively. TG (Tokyo Green)-mAMP: a newly synthesized sensitive ENPP1 fluorescence probe[1].
Aliskiren D6 Hydrochloride is is deuterium labeled Aliskiren, which is a direct renin inhibitor with IC50 of 1.5 nM.
Frovocimab (LY 3015014) is a humanized IgG4 monoclonal antibody (mAb) that neutralizes PCSK9. Frovocimab inhibits PCSK9 binding to LDL receptor (LDLR) while permitting the normal proteolytic cleavage of the bound intact PCSK9[1].
ENPP1-IN-2 is a potent Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) inhibitor with an IC50 value of 32.38 nM for recombinant human ENPP-1. ENPP1-IN-2 has anti-tumor activity[1].
Isoastilbin is a dihydroflavonol glycoside compound in Rhizoma Smilacis glabrae and Astragalus membranaceus. Isoastilbin inhibits glucosyltransferase (GTase) with an IC50 value of 54.3 μg/mL, and also inhibits tyrosinase activity. Isoastilbin shows neuroprotective, antioxidation, antimicrobial and anti-apoptotic properties and has the potential for Alzheimer’s disease research[1][21][3].
Rosuvastatin D3 Sodium is deuterium labeled Rosuvastatin, which is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM.
Ganodermanondiol is a melanogenesis inhibitor isolated from the Ganoderma lucidum[1].Ganodermanondiol exhibits potent cytoprotective effects on tert-butyl hydroperoxide-induced hepatotoxicity[2]. Ganodermanondiol shows significant anti-HIV-1 protease activity with an IC50 of 90 μM[3]. Ganodermanondiol exhibits a strong anticomplement activity against the classical pathway of the complement system with an IC50 of 41.7μM[4].
Brinzolamide(AL 4862) is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM.Target: carbonic anhydrase IIBrinzolamide (< 1 mg) ophthalmic suspension lowers intraocular pressure in Dutch-belted pigmented rabbits in a dose-dependent manner with an onset within 0.5 hour and a peak response by 1-2 hours. Brinzolamide (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours. Brinzolamide dosages of 30 mg/kg, produces a 44% reduction in intestinal charcoal meal progression, but 1 and 10 mg/kg produced 8% and 18% decreases, respectively, in male CD-1 mice. Brinzolamide of 1 mg/kg, 10 mg/kg, and 30 mg/kg prolongs barbiturate sleep time by 57%, 15%, and 35%, respectively, in male CD-1 mice [1]. Brinzolamide (< 3%) produces significantly greater mean percent intraocular pressure reductions and mean intraocular pressure reductions compared with placebo in patients with primary, open-angle glaucoma or ocular hypertension. The optimal intraocular pressure-lowering concentration of brinzolamide is 1%, brinzolamide 1% is well tolerated by patients with primary open-angle glaucoma or ocular hypertension when administered twice daily [2].
IDO1-IN-22 (Compound 3) is a IDO1 inhibitor (biochemical hIDO1 IC50: 67.4 nM, HeLa hIDO1 IC50: 17.6 nM). IDO1-IN-22 has excellent antitumor efficacy in LLC xenograft model, as well as desirable pharmacokinetic (PK) profile[1].
Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC50 of 71.8 nM.
BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 0.9 μM[1].
Atorvastatin sodium is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin sodium inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively[1][2][3][4][5].
Prenyl-IN-1 is a protein prenylation inhibitor, especially a geranylgeranyltransferase (GGT) or a farnesyltransferase (FT) inhibitor, exhibiting potent activity against oxidative stress, and particularly in the treatment of Parkinson's Disease.
Speract, a sea urchin egg peptide that regulates sperm motility, also stimulates sperm mitochondrial metabolism.
MAO A/HSP90-IN-1 (4-b) is a MAO A/HSP90 dual inhibitor with IC50 value of 1.77 μM and 0.019 μM in Glioblastoma (GBM) GL26 cells and HSP90α, respectively. MAO A/HSP90-IN-1 (4-b) can inhibit MAO A activity, HSP90 binding and the expression of HER2 and phospho-Akt to inhibit the growth of GBM, they also reduce PD-L1 expression, which inhibits T cell activation. MAO A/HSP90-IN-1 (4-b) have potential to inhibit tumor immune escape. MAO A/HSP90-IN-1 (4-b) can be used for brain tumor-related diseases research[1].
116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor. 116-9e inhibits Simian Virus 40 (SV40) replication and DNA synthesis. 116-9e inhibits tumor antigen (TAg)’s endogenous ATPase activity and the TAg-mediated activation of Hsp70[1][2].
Perindoprilat (S 9780) is an angiotensin-converting enzyme (ACE) inhibitor with the IC50 value ranging from 1.5 to 3.2 nM. Perindoprilat can be used in hypertension research[1][2].
NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a Kd of 640 nM. NU223612 potently degrades the IDO1 protein through CRBN-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB)[1].