AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM. AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes[1][2].
EGFR-IN-68 (Compound 8d) is a potent EGFR inhibitor with an IC50 of 0.33 μM. EGFR-IN-68 shows anticancer activity[1].
Lodenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED), with less oral bioavailability than Lodenafil carbonate[1].
Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 µM) and GSK-3β (IC50=1.5 µM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research[1][2].
ASP5878 is an oral active and selective inhibitor of the fibroblast growth factor receptor (FGFR), with an IC50 of 3.5 nM for fibroblast growth factor receptor 4 kinase activity. ASP5878 has potential antineoplastic activity[1].
URAT1 inhibitor 5 (compound 16) is a potent URAT1 inhibitor. URAT1 inhibitor 5 can be used in research of hyperuricemia[1].
Isogosferol ((+)-Isogospherol; Isogospherol) is a potent anti-inflammatory agent. Isogosferol decreases LPS (HY-D1056)-stimulated NO and IL-1β expression. Isogosferol decreases the LPS (HY-D1056)-stimulated expression of iNOS, COX-2, NF-κB, and pERK1/2[1].
m-Chloramphenicol (m-threo-Chloramphenicol) is an impurity of Chloramphenicol. Chloramphenicol, a broad-spectrum antibiotic, acts as a potent inhibitor of bacterial protein biosynthesis[1].
S-Methylglutathione is an S-substitued glutathione and a stronger nucleophile than GSH[1]. S-Methylglutathione has inhibitory effect on glyoxalase 1[2].
ML-191 is an antagonist of GPR55. It inhibits GPR55 signaling induced by lysophosphatidylinositol (EC50=1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC50=328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM[1].
PKF050-638 is a potent and selective inhibitor of HIV-1 Rev (IC50=0.04 μM). PKF050-638 inhibits the CRM1-mediated Rev nuclear export by disrupting CRM1-NES interaction[1].
Phaseollin is an isoflavonoid phytoalexin that can be isolated from Phaseolus vulgaris . Phaseollin is toxic to bean hypocotyl and endocarp cells, and causes a complete lysis of sheep erythrocytes[1].
Alfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) is a non-selective VDR activator medication. IC50 value: Target: VDR activatorAlfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) improves mechanical bone strength and bone mass; suppresses osteoclastic bone resorption in vivo.
AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC50 of 0.16 μM for human Nav1.7.
Arimoclomol maleate is a co-inducer of heat shock proteins (HSP).
COX-2-IN-26 is a potent, selective and orally active COX-2 inhibitor with IC50 values of 10.61, 0.067, 1.96 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-26 shows anti-inflammatory activity. COX-2-IN-26 shows gastrointestinal safety profile[1].
Pomstafib-2 is a potent and selective STAT5b inhibitor. Pomstafib-2 decreases the expression of pSTAT5b and induces Apoptosis[1][2].
Paecilomide is a pyridone alkaloid and acetylcholinesterase inhibitor[1].
6-Methoxy-2-[2-(3′-methoxyphenyl)ethyl]chromone (compound 12) is a chromenone[1].
Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively[1].
Fmoc-Asp(OtBu)-Osu is an aspartic acid derivative[1].
BA 41899 is a purely calcium-sensitizing agent. BA 41899 is completely devoid of phosphodiesterase (PDE) III inhibitory activity or any other known inotropic mechanism. BA 41899 can be used for the research of cardiovascular diseases, such as congestive heart failure (CHF)[1].
Sirtuin modulator 4 (compound 12) is a sirtuin modulator. Sirtuin modulator 4 shows inhibitory effect to SIRT1 with an EC50 value of 51-100 μM. Sirtuin modulator 4 may be used for the research of increasing the lifespan of a cell, and preventing a wide variety of diseases and disorders including, for example, diabetes, obesity, neurodegenerative diseases, cardiovascular diseases, inflammation and cancer[1].
H-Pro-Phe-Thr-Arg-Asn-Tyr-Tyr-Val-Arg-Ala-Val-Leu-His-Leu-OH is an peptide. H-Pro-Phe-Thr-Arg-Asn-Tyr-Tyr-Val-Arg-Ala-Val-Leu-His-Leu-OH can be used for the research of various biochemical studies[1].
Itch-Targeting Compound 1 is an anti-itching agent.
GDC-0339 is a Pim kinase inhibitor with IC50 of 43.6 nM for BaF3 PIM1.IC50 value: 43.6 nM (for BaF3 PIM1), 0.04 nM (Ki, for PIM1 LC-3K)Target: Pim
(2-Pyridyldithio)-PEG4-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells[1]. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation[2].
Olmesartan medoxomil-d6 (CS 866-d6) is the deuterium labeled Olmesartan medoxomil. Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM[1][2].