4-Chloro-α-cyanocinnamic acid (α-CHCA) is a classic monocarboxylate transporters (MCT) inhibitor. α-cyano-4-hydroxycinnamate (CHC) has a 10-fold selectivity for MCT1 compared to other MCTs.
BMS-986205 is a selective indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor.
kira6 is a potent type II IRE1α kinase inhibitor with an IC50 of 0.6 μM. It dose-dependently inhibits IRE1α(WT) kinase activity, XBP1 RNA cleavage, Ins2 RNA cleavage and oligomerization.
ONC212, a fluorinated-ONC201 analogue, is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.
GO-203 is a D-amino acid cell-penetrating peptide inhibitor of MUC1-C dimerization and thereby its oncogenic function.
SR9009 is a synthetic REV-ERB agonist with IC50s of 670 nM and 800 nM for REV-ERB-α and for REV-ERB-β, respectively.
ML221 is a potent apelin receptor (APJ) functional antagonist in cell-based assays that is >37-fold selective over the closely related angiotensin II type 1 (AT1) receptor. The IC50 values of ML221 are 0.70 and 1.75 μM in a cAMP assay and β-arrestin assay, respectively.
Verinurad (RDEA3170) is a high-affinity inhibitor of the URAT1 transporter with an IC50 of 25 nM for inhibiting transport activity of human URAT1. It inhibits the related URAT1 homologs OAT4 and OAT1 with approximately 200-fold lower affinity compared to URAT1 with IC50 values of 5.9 µM and 4.6 µM, respectively.