Apoptosis

AZD4877 is another isostere to Ispinesib and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.

ARI-1 is an inhibitor of receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor.

Custirsen sodium inhibits the production of clusterin , an antiapoptotic protein that is upregulated in response to chemotherapy and that confers treatment resistance.

Danvatirsen sodium is an antisense oligonucleotide targeting STAT3 with potential antitumor activity.

JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC).

EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2).

SIAIS164018 drochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively.

Misetionamide is an orally oxathiazin-like compound.

VPC-70063 is a potent Myc-Max inhibitor with an IC50 value of 8.9 μM for Myc-Max transcriptional activity inhibition.

PBENZ-DBRMD is a potent iodotronine deiodinase type 3 (DIO3) inhibitor.

KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively.

U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells.

SFI003 is a SRSF3 inhibitor that drives CRC cell apoptosis via the SRSF3/DHCR24/ROS axis and exhibits potent antitumor effects both in vitro and in vivo.

M47 is a small molecule that selectively destabilizes Cryptochrome 1 (CRY1) and increases degradation of the CRY1 in the nucleus.

MTR-106 is a potent and orally active G-quadruplex stabilizer and RNA polymerase I inhibitor.

TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 µM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively.

ROS-generating agent 1 (Compound 2c) covalently modifies the Sec-498 residue of TrxR to generate ROS.

PRDX1-IN-1 is a selective inhibtor of PRDX1 with an IC50 value of 0.164 μM.

MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization.

BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7.

PH14 is a dual PI3K/HDAC inhibitor with IC50 values of 20.3 nM and 24.5 nM for PI3Kα and HDAC3, respectively.

ABBV-467 is a selective MCL-1 inhibitor (Ki: <0.01 nM).

PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively.

EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively.