PTD10 is a highly potent BTK PROTAC degrader with DC50 of 0.5 nM in TMD8 cells, inhibits cell growth and induces apoptosis more potently than parent molecule GDC-0853.

PROTAC dCE-1 is a potent, selective CBP/EP300 degrader targeting the histone acetyltransferase (HAT) domain, with DC50 value of 1.3 μM in LP1 cells.

PIK5-12d is a highly potent, selective, first-in-class PIKfyve PROTAC degrader, potently degrades PIKfyve protein with DC50 value of 1.48 nM and Dmax value of 97.7% in prostate cancer VCaP cells.

MTX-23 is a proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) splice variant-7 (AR-V7) and AR-full length (AR-FL) with DC50 of 0.37 and 2 uM, respectively.

MS3227 is a proteolysis-targeting chimera (PROTAC) that targets MDM2 by recruiting the E3 ligase VHL, resulting in proteasome-dependent degradation of MDM2.

MS147 (MS 147) is the first degrader of PRC1 core components, BMI1 and RING1B, comprises an EED small-molecule binder (EED226, Cat. PC-42321) linked to a ligand of the E3 ligase von Hippel-Lindau (VHL), degrades BMI1/RING1B in an EED-, VHL-, ubiquitinatio

MS132 is a highly potent and selective VHL-recruiting WDR5 PROTAC degrader with DC50 of 92 nM in MIA PaCa-2 cells.

LL-K8-22 is a potent, selective dual degrader of of CDK8 and cyclin C (MDA-MB-468 cell DC50, 2.52 and 2.64 uM), significantly degrades CDK8 without reducing CDK19 and does not degrade other cyclin proteins.

KYH1872 is a PROTAC that induces protein degradation via the KLHDC2 E3 ubiquitin ligase, KYH1872 is consisted of a C-terminal fragment of the SelK protein and promiscuous kinase inhibitor YHJ1039 via PGE linker.

JWZ-1-80 is a potent and selective PROTAC degrader of PI5P4Kγ with Kd of 510 nM, 1 uM induces 75% reduction of PI5P4Kγ in Molt4 cells.

JH-XII-03-02 is a highly potent, selective PROTAC degrader of LRRK2 with IC50 of 1 nM against both wt LRRK2 and LRRK2 G2019S.

JET-209 (JET209) is a potent, selective PROTAC degrader of CBP/p300 based on GNE-207 with DC50 of 0.05 nM for CBP and 0.2 nM for p300, Dmax >95% for both proteins in the RS4;11 leukemia cell line.

JCS-1 is a RG3039-based degarder (PROTAC) of the RNA decapping scavenger protein DcpS exhibiting effective degradation of DcpS at nanomolar concentrations, non-covalently binds DcpS and recruits the E3 ligase VHL, induces potent, rapid, and sustained DcpS

INY-06-061 is a potent and selective heterobifunctional degrader of ERK5 with binding Kd of 12 nM and DC50 of 21 nM in MOLT4 cells (5h treatment).

HPP-9 is a potent BET bromodomain degrader that acts through a PROTAC mechanism, HPP-9 is a long-acting Hedgehog pathway inhibitor.

DU-14 is a highly potent and selective small molecule degrader for both PTP1B and TC-PTP with DC50 values of 4.3 and 4.8 nM, respectively, in HEK293 cells after 16 hours treatment.

Degradomer D-1 is a selective proteasomal degrader of IRAK3 with Kd of 100 nM, DC50 of 94 nM, displays no binding affinity against IRAK4 (Ki >10 uM).

DeFer-2 is an oleic acid (OA)-based ferritin-targeting PROTAC binding Kd of 17.1 uM, degrades ferritin and rapidly elevates the free iron content, induces pyroptosis.

dEALK1 is a small-molecule degrader of EML4-ALK fusion proteins with binding constant (Kd) value of 44 nM for kinase domain of recombinant ALK, overcomes resistance to ALK inhibitor ceritinib.

DBt-10 is a potent BTK-specific DCAF1 PROTAC with TR-FRET IC50 of 136 nM, potently degrades BTK with DC50 of 137 nM in TMD8 BTK-GFP/mCherry cell-based assays.

DB0614 is a CRBN-based PROTAC, induces the degradation of NEK9, FAK, CDK4, CDK6, and WEE1 in cells.

DAS-CHO-5-oCRBN is a potent and selective PROTAC for c-Src kinase with DC50 value of 62 nM in CAL148 cells.

DAS-5-oCRBN is a potent and selective PROTAC for c-Src kinase with DC50 value of 3 nM, without effect on Bcr-Abl.

CRBN(FLT3)-8 a highly potent FLT3 degrader by introducing gilteritinib into targeted protein degradation technology, potently degrades FLT3-ITD via UPS and inhibits the proliferation of FLT3-ITD mutant AML cells more effectively than gilteritinib.

CRBN(BRAF)-24 is a potent small molecule degrader against oncogenic BRAF V600E protein, potently degrades BRAFV600E in a ubiquitin–proteasome system (UPS)-dependent manner and inhibits the proliferation of BRAFV600E-driven cancer cells.

Chk1 PROTAC-2 is a potent Chk1 degrader with DC50 of 1.33 µM in A375 cells.

BWA-522 is a potent, orally bioavailable PROTAC degrader of the androgen receptor N-terminal domain (AR-NTD), induces AR-FL or AR-V7 protein degradationwith DC50 of 0.73 μM (AR-FL) and 0.67 μM (AR-V7) in VCaP cells.

BTX-6654 is a potent, selective SOS1 cereblon-based bifunctional PROTAC degrader, reduces downstream signaling markers, pERK and pS6, and displayed antiproliferative activity in cells harboring various KRAS mutations.

BSJ-04-146 is a potent, selective FAK PROTAC (IC50=26 nM), induces potent and durable FAK degradation in pancreatic and breast cancer cell lines at 10 nM.

BJG-05-039 is a PAK1-selective degrader consisting of NVS-PAK1-1 conjugated to lenalidomide, a recruiter of the E3 ubiquitin ligase substrate adaptor Cereblon.