PU-H71 is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells.
KU-32 is a novel, novobiocin-based Hsp90 inhibitor that can protect against neuronal cell death.
N-Arachidonyl maleimide is a potent, irreversible inhibitor of monoacylglycerol lipase (MAGL) with an IC50 value of 140 nM[1].
Rubrofusarin 6-O-β-D-glucopyranoside, the glycoside of Rubrofusarin, is a protein tyrosine phosphatase 1B (PTP1B) inhibitor with the IC50 of 87.36 μM. Rubrofusarin 6-O-β-D-glucopyranoside can be used for the research of comorbid diabetes and depression[1].
Cassiaside B2 is a protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A) inhibitor. Cassiaside B2 possesses antiallergic and is a 5-HT2C receptor agonist[1][2].[3]..
CYP3A4-IN-3 is a high-affinity specific inhibitor of cytochrome P450 3A4 (CYP3A4) with the IC50 value of 0.075 μM. CYP3A4-IN-3 is a ritonavir analogue, but with a simpler structure and twice the inhibitory effect of ritonavir. CYP3A4-IN-3 is used as an antiviral agent and immunosuppressant[1].
MT-3014 is a potent, highly selective and brain-penetrated phosphodiesterase 10A (PDE 10A) inhibitor, with IC50s of 0.062 nM and 0.09 nM for human PDE 10A and bovine PDE 10A, respectively[1].
Quinapril-d5 hydrochloride (CI-906-d5) is the deuterium labeled Quinapril hydrochloride. Quinapril hydrochloride (CI-906) is a prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications[1][2].
(E/Z)-HA155 is a potent autotaxin (ATX) type I inhibitor. (E/Z)-HA155 can be used for researching cancer, fibrotic diseases, inflammation, pain and angiogenesis[1].
SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.
Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.
(R)-(-)-Rolipram is the R-enantiomer of Rolipram. Rolipram is a selective inhibitor of phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.
D609 is a selective competitive inhibitor of phosphatidyl choline-specific phospholipase C (PC-PLC), with Ki of 6.4 μM.
Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain[1].
6-Fluorotryptophan, a competitive inhibitor of tryptophan hydroxylase, produced a transient disruption of sleep in rats chronically implanted with EEG recording electrodes[1].
Ralpancizumab is a selective PCSK9 inhibitor with potential application in hemorrhagic stroke[1].
NC1 is a novel highly active allosteric inhibitor of protein tyrosine phosphatase, non-receptor type 22 (PTPN22) which is a lymphoid-specific tyrosine phosphatase (LYP).
Revizinone is a novel selective phosphodiesterase (PDE) inhibitor with IC50 values on this enzyme to 0.036 microM. target: phosphodiesterase (PDE)[3]; IC 50: 0.036 microM; [3]In vivo: The administration of Revizinone improved the haemodynamic profile with an increase in cardiac output, a decrease in systemic vascular resistance and a stable heart rate and mean arterial blood pressure. [1] With regard to reconstitution of contractility and cardiac function Revizinone (E-isomer) was 10 fold more potent than R 79595 and nearly 100 fold more potent than R 80123 (Z-isomer). [2] Revizinone significantly increased global LV function and systolic wall thickening in ischemic areas at doses greater than or equal to 0.16 mg/kg i.v. [4]
Suc-AAPR-pNA is a substrate of trypsin acyl-enzymes. Suc-AAPR-pNA can be used to test trypsin acyl-enzymes activity[1][2].
Safusidenib is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma[1]. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively[2].
LDCA is a dual-hit metabolic modulator and inhibits LDH-A enzyme activity to stimulate apoptosis in the malignant population. LDCA can be used for the research of oncogenic progression[1].
AMPD2 inhibitor 1 is an adenosine monophosphate deaminase 2 (AMPD2) inhibitor, used in the research of sugar craving, salt craving, umami craving, and addictions including drug, tobacco, nicotine and alcohol addictions.
Triolein-d5 is the deuterium labeled Triolein. Triolein is a symmetrical triacylglycerol, reduces MMP-1 upregulation, with strong antioxidant and anti-inflammatory properties[1].
Nevanimibe (PD-132301; ATR101) is a selective and potent acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe (PD-132301; ATR101) inhibits ACAT2 with an EC50 of 368 nM[1].
Okadaic acid is extracted from black sponges of the genus Halichondria. Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A and PP3 inhibitor with IC50s of 10-15 nM, 0.5 nM and 4 nM, respectively.[1][2] Okadaic acid eliminate metazoan symbionts/parasites by apoptosis[3].
Kojic acid dipalmitate (Kojic dipalmitate) is a derivative of Kojic acid (HY-W050154), a fungal metabolite that can be produced by species of Aspergillus, Acetobacter and Penicillium. Kojic acid dipalmitate is a slow and reversible competitive inhibitor of tyrosinase. Kojic acid dipalmitate can be used for skin‐lightening agent research[1].
NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties.
CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
BAY 87-2243 is a highly potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor.
Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.