Tetrazine-PEG6-amine (hydrochloride) is a cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Amino-PEG4-bis-PEG3-propargyl is a cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

A metabolite of Flurazepam Controlled substance (depressant).

LC-2 is a potent and first-in-class degrader of endogenous KRAS G12C with DC50 values between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines.

CS-3150 (Esaxerenone, XL-550) is a highly potent, selective and orally active non-steroidal mineralocorticoid receptor antagonist with IC50 of 9.4 nM; displays >1,000-fold selectivity over other steroid hormone receptors, glucocorticoid receptor, androgen receptor and progesterone receptor; inhibits aldosterone-induced transcriptional activation of human mineralocorticoid receptor with IC50 of 3.7 nM, shows superior potency to that of spironolactone and eplerenone; suppresses aldosterone-induced decrease in urinary Na(+)/K(+) ratio, inhibits blood pressure elevation induced by DOCA/salt-loading in rats.

Selective blocker of the Aquaporin-1 ion channel conductance, slowing cancer cell migration

LEM-14 is a specific inhibitor of histone lysine methyltransferase NSD2 (MMSET/WHSC1) with in vitro IC50 of 132 uM, and that is inactive against the closely related NSD1 and NSD3..

Bractoppin is a potent, small-molecule chemical inhibitor that specific selectively blocks phosphopeptide recognition by the BRCA1 tBRCT domain with binding IC50 of 74 nM; shows no inhibition for recognition of cognate biotinylated phosphopeptides to the TOPBP1 tBRCT 7/8, or GRB2 SH2 proteins; engages BRCA1 tBRCT residues recognizing pSer in the consensus motif, pSer-Pro-Thr-Phe, plus an abutting hydrophobic pocket; inhibits substrate recognition detected by Förster resonance energy transfer, and diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51; selectively interrupts BRCA1 tBRCT-dependent signals evoked by DNA damage.

LDC195943(IMT1) is a highly specific inhibitor of human mitochondrial RNA polymerase (POLRMT).

Novel inhibitor of the VP40 matrix protein

PU-H54 is potent, selective Grp94 inhibitor.

Positive Allosteric Modulators (PAMs) of mGlu5 with Competitive MPEP-Site Interaction

Potent, reversible, and ATP-competitive inhibitor of human Thymidylate kinase (TMPK)

Inhibitor of placental alkaline phosphatase (PLAP)

Talinolol is a beta(1)-adrenergic receptor antagonist and a probe drug for P-glycoprotein (P-gp) activity in humans.

hPGDS-IN-1 is a potent, selective hPGDS inhibitor with IC50 of 12 nM in FP or EIA assays..

α-Adrenergic blocker

A discontinued antiemetic drug used in post-operative care

Novel NMDA receptor antagonist

Novel non-toxic fluorescent probe to label the renal proximal tubules in zebrafishReference1) The small molecule probe PT-Yellow labels the renal proximal tubules in zebrafish; Chem Commun (Camb). 2015;51(2):395-8. doi: 10.1039/c4cc08075k. Epub 2014 Nov 1

Novel ligand for the Methyl-lysine Binding Protein, 53BP1.

Novel highly potent BET bromodomain inhibitor with more than 100-fold higher cellular potency than the corresponding monovalent antagonist JQ1

Anti-inflammatory drug