The single isomer, 5-FAM, contains a carboxylic acid that can be used to react with primary amines via carbodiimide activation of the carboxylic acid. Fluorescein is the most common fluorescent derivatization reagent for labeling biomolecules. In addition

The RS-isomer of LOXO-195, a potent, selective, next-generation Trk tyrosine kinase inhibitor with IC50 of 0.6 nM and <2.5 nM for WT TrkA and WT TrKC, respectively..

the R-enantiomer of the nootropic drug oxiracetam (ISF 2522), which is a nootropic drug of the racetam family and stimulant..

The racemate of Pemafibrate, which is a highly potent, specific PPARα agonist with EC50 of 1 nM..

The R racemate of LOXO-195, a potent, selective, next-generation Trk tyrosine kinase inhibitor with IC50 of 0.6 nM and <2.5 nM for WT TrkA and WT TrKC, respectively..

The R form of Bay 65-1942. which is a potent, selective, ATP-competitive inhibitor of IKKβ kinase with Ki of 2 nM..

The R enantiomer of Refametinib, a potent, non–ATP-competitive, highly selective, allosteric inhibitor of MEK1/2 with IC50 of 19/47 nM respectively..

The R enantiomer of GLPG-0492, a non-steroidal selective androgen receptor modulator (SARM) for treatment for Duchenne muscular dystrophy (DMD).

The prodrug of TG 100572, a potent, dual receptor tyrosine kinase/Src kinase inhibitor with IC50 of 2-16 nM for VEGFR, FGFR and PDGFR, 0.1-5 nM for Src family.

The prodrug of PF-04928473 (SNX-2112), a potent, orally bioavailable HSP90 inhibitor.

The prodrug of cidofovir diphosphate that inhibits cytomegalovirus (CMV) viral replication by selectively inhibiting viral DNA polymerases.

The prodrug of AUDA, a potent inhibitor of sEH (soluble epoxide hydrolase) with IC50 of 50 nM and 100 nM for mouse sEH and human sEH, respectively.

The pivaloyloxymethyl ester prodrug of Stafib-2, which is a potent, selective STAT5b inhibitor with Ki of 9 nM.

The orally bioavailable prodrug of Galiellalactone, a direct inhibitor of STAT3, prevents the transcription of STAT3 regulated genes.

The orally active prodrug of candoxatrilat (UK-73967), potent neutral endopeptidase EC 3.4.24.11 (atriopeptidase) inhibitor..

The more active enantiomer of (±)-U-50488, a potent, selective kappa-opioid receptor agonist with no μ-opioid antagonist effects.

The L-lysylamide prodrug of 5F-203 (NSC703786), a potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway.

The intermediate of ARS-853.ARS-853 is a selective, covalent inhibitor of KRAS-G12C that inhibits mutant KRAS driven signaling by binding to the GDP bound oncoprotein and preventing activation.

The first small molecule ligand for the VEGF-A receptor neuropilin 1 (NRP1).

The first selective, cell-permeable inhibitor of GAG sulfotransferases with IC50 of 2.0-2.5 uM .

The first potent and selective proton-sensing GPCR GPR4 antagonist with IC50 of 67 nM, with no activity against TDAG8 and OGR1 (IC50>10 uM).

The distomer of BRS-3 agonist Compound A, shows no activity for bombesin receptor subtype-3 (BRS-3) with EC50>10 uM..

The dimethyl ester of N-oxalyl-d-phenylalanine (NOFD), a specific HIF asparaginyl hydroxylase (FIH) inhibitor with Ki of 83 uM, but not HIF prolyl hydroxylase (>1 mM).

The cell-permeable, pivaloyloxymethylester of Stafib-1, which is a potent, selective small molecule inhibitor of transcription factor STAT5b with Ki of 44 nM, >50-fold selectivity over STAT5a.

The calcium salt of levomefolic acid that has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers. .

The antiglucocorticoid RU43044 exerted significant agonist activity and activated MMTV-Luc transcription in osteosarcoma cells but not human breast cancer cells.

The (1R,2R) diastereomer of 2-PCCA, a potent, selective agonist of the orphan GPR88 receptor with EC50 of 373 nM, 5-fold more potent than the (1S, 2S)-isomer..

Thalidomide-O-amido-C3-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

TH 5427 (TH5427) is a potent, small molecule NUDT5 (NUDIX5) inhibitor with IC50 of 29 nM, 690-fold selectivity for NUDT5 over MTH1 (NUDT1) in vitro.

TGR-1202 R-enantiomer is is the less active enantiomer of TGR-1202 (Umbralisib), TGR-1202 is a potent, selective, orally available PI3Kδ inhibitor with IC50 of 22 nM..