Fenofibrate is a PPARα agonist with an EC50 of 30 μM.
Cemdomespib (KU-596) is a highly bioavailable second-generation Hsp90 modulator. Cemdomespib has shown efficacy in improving sensory deficits in models of diabetic peripheral neuropathy. Cemdomespib induces Hsp70 levels and manifest neuroprotective activity through induction of the heat shock response[1][2][3].
HCVP-IN-1 (compound 1) is a hepatitis C viral polymerase (HCVP) inhibitor[1].
Validamycin A is an aminoglycoside agricultural antibiotic. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL[1]. Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM[2].
JNJ-61803534 is a potent and orally active RORγt inverse agonist with an IC50 of 9.6 nM. JNJ-61803534 has anti-inflammatory activity. JNJ-61803534 inhibits IL-17A production in human CD4+ T cells under Th17 differentiation conditions[1].
CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases[1][2][3][4].
Delapril is an angiotensin-converting enzyme (ACE) inhibitor for the treatment of cardiovascular diseases[1].
BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity[1].
MG-101 is a potent inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively.
3,3′-Bisdemethylpinoresinol, lignin, is a nature product and has MMP-1 inhibitory activity in UVA-irradiated human dermal fibroblasts. 3,3′-Bisdemethylpinoresinol can be isolated from the seeds of Morinda citrifolia[1].
Incyclinide (CMT-3, COL-3) is a matrix metalloproteinase (MMP) inhibitor, thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis.
Vasicinol is a reversible inhibitor of sucrase (IC50: 250 μM). Vasicinol is a HbF inducer. Vasicinol also inhibits Angiotensin-converting Enzyme (ACE). Vasicinol is apyrroquinazoline alkaloid that can be isolated from Adhatoda vasica[1][2].
PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma.
ATRA-biotin (Biotin-ATRA-conjugate) is a biotin-conjugated ATRA. ATRA-biotin can be used to track ATRA in cells or a given tissue[1].
HS-80 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-80 is able to inhibit the incorporation of tritiated acetate into lipids with an IC50 of 7.13 μM.
MLN4924 is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM.
Deoxycorticosterone acetate is a steroid hormone produced by the adrenal gland that possesses mineralocorticoid activity and acts as a precursor to aldosterone.
Alismanol M is a farnesoid X receptor (FXR) agonist with an EC50 value of 50.25 μM. Alismanol M is a protostane-type triterpenoid that can be isolated from the rhizome of Alisma orientale. Alismanol M can be used for the research of cholestasis and nonalcoholic steatohepatitis[1].
L-731735 is a selective FPTase inhibitor that can inhibit ras-dependent cell transformation. L-731735 can be used in cancer research[1].
2,3,4'-Trihydroxy-3',5'-dimethoxypropiophenone, isolated from Parinari hypochrysea (Chrysobalanaceae), exhibits antioxidant and lipoxygenase inhibition[1].
EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
YG1702 is a potent ALDH18A1-specific inhibitor. YG1702 attenuates the growth of MYCN-amplified NB and down-regulates MYCN. YG1702 physically interacts with ALDH18A1 with a high affinity and might potentially affect its enzymatic activity[1].
Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.IC50 value:Target: Factor Xa Otamixaban is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa. In vivo experiments have demonstrated that Otamixaban is highly efficacious in rodent, canine and porcine models of thrombosis. In addition, recent clinical findings indicate that Otamixaban is efficacious, safe and well tolerated in humans and therefore has considerable potential for the treatment of acute coronary syndrome. This review article chronicles the discovery and pre-clinical data surrounding the fXa inhibitor Otamixaban as well as the recent clinical findings in humans.
Hirudin is a Thrombin inhibitor with blood anticoagulant property. Hirudin has potent anti-thrombotic, wound repair, anti-fibrosis, anti-tumor and anti-hyperuricemia effects. Hirudin also affects diabetic complications, cerebral hemorrhage, and others[1].
(R)-MLN-4760, the R-enantiomer of MLN-4760, is an ACE2 inhibitor, with an IC50 of 8.4 μM. (R)-MLN-4760 is the less active isomer[1].
PD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM).IC50 value: 0.26 ± 0.03 μM (Ki, for μ-calpain), 5.33 ± 0.77 μM (Ki, for m-calpain) [1]Target: calpainin vitro: The μ-calpain inhibitor PD 151746 decreases oxLDL-induced cytotoxicity. [2]
Sulthiame-d4 is the deuterium labeled Sultiame. Sultiame is a carbonic anhydrase inhibitor, widely used as an antiepileptic agent[1][2].
Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity[1]. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC50 of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast cancer[2].
Pravastatin lactone is a potent HMG-CoA inhibitor. Pravastatin Lactone is a metabolite of pravastatin. Pravastatin lactone reduces blood cholesterol levels by inhibiting cholesterol synthesis[1].
Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.