Lonafarnib is an orally bioavailable farnesyl protein transferase (FPTase) inhibitor for H-ras, K-ras and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively.
Isosilybin (Isosilybinin) is a flavonoid from milk thistle; inhibits CYP3A4 induction with an IC50 of 74 μM.
Rosiptor is an activator of SH2-containing inositol-5'-phosphatase 1 (SHIP1).
MMPI-1154 is a small molecule MMP-2 inhibitor with IC50 of 10/6.6/13/1.8 uM for MMP1/2/9/13, respectively; shows significant cardio-cytoprotecion, significantly decreases infarct size when applied at 1 μM in an ex vivo model for acute myocardial infarction.
Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM.
CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 12 nM.IC50 value: 12 nMTarget: cPLA2CAY10650 is a highly potent (IC50 = 12 nM) cPLA2α inhibitor. It demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis. Chinese hamsters (n = 6/group) were infected with parasite-laden contact lenses and treated with cPLA2α inhibitors (AACOCF3 and CAY10650) 50 μg/5 μl was injected with topical eye-drop under the contact lens of an infected cornea three times a day for 6 days and topically on days 7–14 postinfection. Animals were anesthetized and sacrificed 15 days after application of cPLA2α inhibitors. Treatment with the AACOCF3 and CAY10650 had a profound effect on the severity and chronicity of keratitis. In addition, hamsters treated with AACOCF3 had significantly less severe keratitis as compared with CAY10650 group.
LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.
Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) . Apratastat can potently inhibit the release of TNF-α in vitro, ex vivo, and in vivo with IC50s of 144 ng/mL in vitro and 81.7 ng/mL ex vivo, respectively[1].
TAK-243 is a potent and selective ubiquitin-like modifier activating enzyme 1 (UBA1) inhibitor.
Dnp-GPLGMRGL-NH2 is a peptide substrate for matrix metalloproteinase-13 (MMP-13) with a kcat/Km value of 4,200,000 M-1s-1.
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria[2]. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level[1].
TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP[1].
Tropolone, a tropone derivative with a hydroxyl group in the 2-position, is a precursor of manyazulene derivatives such as methyl 2-methylazulene-1-carboxylate[1]. Tropolone is a potent inhibitor of mushroom tyrosinase with a IC50 of 0.4 μM, and the inhibition can be reversed by dialysis or by excess CU2+[2].
Rpn11-IN-1 is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.
SC-22716 is a potent, competitive, reversible inhibitor of human LTA4 hydrolase, with an IC50 of 0.20 µM. SC-22716 has potential for the research of inflammatory bowel disease (IBD) and psoriasis[1].
Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease[1][2].
Enprofylline acts as a selective and competitive A2B receptor antagonist with the Ki of 7 μM. Enprofylline also acts as a phosphodiesterase inhibitor. Enprofylline can be used for the research of asthma, chronic obstructive pulmonary disease[1][2][3].
Z-Leu-Leu-Glu-AMC is a substrate peptide, and can be used for determination of postacidic-like hydrolysing activity of 20S proteasome[1]
Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P4503A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults[1][2][3].
Methazolamide is a carbonic anhydrase inhibitor used to treat glaucoma.Target: Carbonic AnhydraseMethazolamide is a carbonic anhydrase inhibitor with Ki of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively [1]. Methazolamide is of strength equal to acetazolamide, another carbonic anhydrase inhibitor used to treat irregular breathing disorders. However, methazolamide differs from acetazolamide in that it fails to activate Ca2+-dependent potassium channels in skeletal muscles. Methazolamide does not impair respiratory work performance in anesthetized rabbits [2]. Oral administration of methazolamide decreases IOPs and AHFRs in clinically normal dogs, with effectiveness diminishing in the evening [3].
Z-Arg-Arg-pNA is a substrate for cathepsin B and can be used to detect this enzyme activity[1].
ACC1/2-IN-1 (compound 4s) is a potent ACC1/2 inhibitor with IC50 values of 98.06 and 29.43 nM for ACC1 and ACC2, respectively. ACC1/2-IN-1 can be used for cancer research[1].
Aleplasinin is an orally active, potent, BBB-penetrated and selectiveSERPINE1 (PAI-1, Plasminogen activator inhibitor-1) inhibitor. Aleplasinin increases amyloid-β (Aβ) catabolism and ameliorates amyloid-related pathology. Aleplasinin improves memory deficiency. Aleplasinin can be used for Alzheimer's disease research[1][2].
CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug metabolism[1].
CD2314 is a potent and selective RARβ receptor agonist with a Kd of 195 nM in S91 melanoma cells[1].
Doxycycline monohydrate is an antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor[1][2][3][4].
Hsp90-IN-17 (Example 5) is an HSP90 inhibitor that can be used in the study of proliferative diseases, such as cancer and neurodegenerative diseases[1].
Elvitegravir is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
Deserpidine (Harmonyl) is an alkaloid isolated from the root of Rauwolfia canescens related to Reserpine. Deserpidine is used as an antihypertensive agent and a tranquilizer. Deserpidine is a competitive angiotensin converting enzyme (ACE) inhibitor. Deserpidine also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex[1][2][3].