Tanshinone I is an inhibitor of type IIA human recombinant sPLA2 (IC50=11 μM) and rabbit recombinant cPLA2 (IC50=82 μM).
IDO1-IN-18 (Compound 14) is a potent inhibitor of IDO1. IDO1-IN-18 has the potential for the research of cancer diseases[1].
GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.
A potent, selective, orally active inhibitor of cathepsin K with Ki of 0.1 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively; shows less or no potentcy for human cathepsin S/L/B/C (Ki=0.83/1.7/32/2500 nM); inhibits human osteoclasts bone resorption in vitro at a concentration more than 100 fold lower than that of alendronate; reduces plasma calcium level increased by PTHrP in thyroparathyroidectomized rats, decreases serum and urine C-telopeptide of type I collagen level. Osteoporosis Phase 2 Discontinued
Nidufexor is a farnesoid X receptor (FXR) agonist[1].
Carbonic anhydrase inhibitor 14 (Compound 8b) is a carbonic anhydrase (CA) inhibitor with Ki values of 1203, 99.7, 9.4 and 27.7 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. Carbonic anhydrase inhibitor 14 can also inhibit CDK2 with an IC50 of 20.3 μM. Carbonic anhydrase inhibitor 14 shows antitumor activity[1].
Tetrahydroamentoflavone (Amentoflavanone) is a potent xanthine oxidase (XO) inhibitor. Tetrahydroamentoflavone has inhibitory activity for XO with IC50 and Ki values of 92 nM and 0.982 μM, respectively. Tetrahydroamentoflavone can be used for the research of inflammatory disorders and gout[1].
BMS-309403 is a potent, selective and cell-permeable inhibitor of fatty acid binding protein 4 (FABP4) with a Ki of less than 2 nM.
Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.Target: ACERamipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM [1]. Ramipril enhances the activity of ACE-associated CK2 and the phosphorylation of ACE Ser1270 in cultured endothelial cells, but is unable to activate JNK or stimulate the nuclear accumulation of c-Jun in endothelial cells expressing a S1270A ACE mutant or in ACE-deficient cells. Prolonged Ramipril treatment increases ACE expression in primary cultures of human endothelial cells and in vivo (mouse lung), which can be prevented by pretreatment with the JNK inhibitor SP600125 [2].Chronic in vivo administration of Ramipril to rats at a dosage that has similar hypotensive effects in vitro HUVECs significantly reduces the rate of LPS-induced apoptosis compared to the other ACE inhibitors, which contrasts with the apoptosis effect in vitro [3]. Ramipril inhibits systolic blood pressure (SBP) with IC50 of 1.97 mg/kg in spontaneously hypertensive rats (SHR). When in combination with AT1-receptor blockade by candesartan-cilexetil increases SBP reduction synergistically rather than additively [4].
Sofigatran (MCC-977) is an orally active factor IIa (thrombin) inhibitor, acts as an anticoagulant. Sofigatran is used for the research of cardiovascular disease[1].
ACT001 is an orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of DMAMCL (a prodrug of Micheliolide), can cross the blood-brain barrier. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects[1][2].
Daclatasvir is a potent HCV NS5A protein inhibitor, with mean EC50 values of 50 and 9 pM against genotype 1a and 1b replicons, respectively.
Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[2][3][4][5][6][7].
ALDH3A1-IN-2 (Compound 19) is a potent inhibitor of ALDH3A1 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH3A1-IN-2 has the potential for the research of cancer diseases[1].
Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor, which inhibits FAAH with IC50s of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, respectively.
Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide[1].
β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol[1][2][3].
ML-030 is a potent PDE4 inhibitor, with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively.
Homo Sildenafil-d5 is the deuterium labeled Homo Sildenafil. Homo Sildenafil, an analog of Sildenafil, acts as a phosphodiesterase inhibitor[1][2].
Stigmasterol glucoside is a sterol isolated from P. urinaria with high antioxidant and anti-inflammatory activities[1], act as an inhibitor of 5α-reductase with an IC50 of 27.2 µM[2].
C12 NBD sphingomyelin is an active derivative of sphingomyelin (HY-113498) that is tagged with fluorescent C12 nitrobenzoxadiazole (C12 NBD). C12 NBD sphingomyelin can be used as a sphingomyelinase substrate for studying the metabolism and transport of sphingomyelins (Ex=470 nm, Em=525 nm)[1].
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM[1]. Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM[1][2].
Chymostatin is a potent cathepsin G inhibitor. Chymostatin inhibits fungal growth when combined with other pepsin inhibitors. Chymostatin can be used for acute lung injury and pancreatitis research[1].
Licopyranocoumarin is an isoflavonoid that shows CYP3A4 inhibitory activity with an IC50 of 32 μM. Licopyranocoumarin has potent neuroprotective activities[1].
CAY10581, a pyranonaphthoquinone derivative, is a highly specific and reversible uncompetitive IDO Inhibitor with an IC50 of 55 nM[1][2].
Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.
Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity[1] [2][3].
3-O-Acetyl-11-hydroxy-beta-boswellic acid is a potent 5-lipoxygenase (5-LO) inhibitor[1].
CORT 118335 (Miricorilant, C118335) is a novel potent, selective, non-steroidal glucocorticoid receptor (GR) antagonist with Ki of 8 nM, shows modest affinity for MR.