Apoptosis

PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells.

BLU-222 is an orally active and highly selective CDK2 inhibitor.

HA-9104 is a potent and selective inhibitor of cullin-5 neddylation via virtually targeting the V30 pocket of UBE2F.

YSR734 (Compound 21) is a covalent HDAC inhibitor with IC50 values of 110 nM, 154 nM, and 143 nM for HDAC1, HDAC2, and HDAC3, respectively.

BDM19 binds and activates cytosolic BAX dimers, and prompts cell apoptosis either alone or in combination with BCL-2/BCL-XL inhibitor Navitoclax.

WK369 is a novel BCL6 small molecule inhibitor, which exhibits excellent anti-ovarian cancer bioactivity, induces cell cycle arrest and causes apoptosis.

ATPase-IN-3 (compound 6) is a ATPase inhibitor.

BFC1108 is a small molecule Bcl-2 functional converter.

Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively.

SC912 is an AR-V7 inhibitor (IC50 = 0.36 μM).

MY-1442 (I-3) is a microtubulin polymerization inhibitor.

GGTI-2417 is a potent and selective inhibitor of GGTase I.

NSD-IN-3 (compound 3) is a potent nuclear receptor binding SET domain (NSD) inhibitor.

SDU-071 is a potent and orally active inhibitor of BRD4-p53 inhibitor.

XL44, an hRpn13 binder, induces hRpn13-dependent apoptosis and also restricts cell viability by a PCLAF-dependent mechanism.

PROTAC AR/AR-V7 degrader-1 (27c) is a PROTAC-based and dual AR, AR-V7 degrader, with DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively.

TS-24 is an inhibitor for cathepsin S, with an IC50 of 4.3 μM.

SelSA is a selective, orally active inhibitor for histone deacetylase 6 (HDAC6) with IC50 of 56.9 nM.

BPU arrests cell cycle progression in the sub-G1 phase.

ASCT2-IN-1 (compound 20k) is an ASCT2 inhibitor with IC50 values of 5.6 μM and 3.5 μM in cells A549 and HEK293, respectively.

ASCT2-IN-2 (compound 25e) is an ASCT2 inhibitor with IC50 of 5.14 μM.

SpiD3 is a novel spirocyclic dimer.

UR778Br targets the GTPase-activating protein-related domain (GRD domain) of IQGAP1 proteins.

PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader for CDK4 and CDK6 with DC50 of 10.5 and 2.5 nM.