AR ligand 42 is a androgen receptor ligand. AR ligand 42 can be used to synthesize androgen receptor PROTAC degrader ITRI-90.

Pan-KRAS ligand 3 is a pan-KRAS inhibitor. Pan-KRAS ligand 3 can be used for synthesis of PROTAC pan-KRAS degrader-1.

DDR1 ligand 1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). DDR1 ligand 1 can be used for the synthesis of PROTAC DDR1 degrader-1.

UR241-2 is an IRAK4 inhibitor. UR241-2 suppresses IL-1–induced IRAK1/4 signaling, NF-κβ activation, and phosphorylation of p65 and p38. UR241-2 selectively inhibits leukemia stem cell clonogenicity. UR241-2 can serve as a ligand for target proteins for PROTAC, facilitating the development and design of PROTAC degraders for IRAK4. UR241-2 can be used in the research of acute myeloid leukemia.

AR-DBD ligand-1 is an AR-DBD ligand. AR-DBD ligand-1 can be used to synthesize PROTAC LYA914.

TH10184 is a NUDT5 inhibitor. TH10184 can be conjugated with VH032 and linker to synthesize PROTAC NUDT5 degrader DDD2

BCL6 ligand-5 (Compound 37) is a BCL6 ligand. BCL6 ligand-5 can be used as a ligand for target protein for PROTAC to develop and design degraders for PROTAC BCL6, such as PROTAC BCL6 Degrader-2. BCL6 ligand-5 can also be used in tumor research.

BTK/IKZF1/3 ligand 1 is a BTK/IKZF1/3 PROTAC ligand. BTK/IKZF1/3 ligand 1 can be conjugated with E3 ligase Ligand and linker to synthesize PROTAC BTK/IKZF1/3 Degrader-1. PROTAC BTK/IKZF1/3 Degrader-1 can be used for cancer research.

Multi kinase ligand 4 is a target protein ligand used in the synthesis of PROTAC DB-0646.

HPK1 ligand 6 is a HPK1 ligand. HPK1 ligand 6 can be used to synthesize PROTAC HPK1 Degrader-6.

FTO ligand-1 is a FTO ligand for FTO PROTAC degrader FP54. FTO ligand-1 can inhibit cell proliferation and block the FP54-induced FTO degradation. FTO ligand-1 can be used for research of cancer, such as acute myeloid leukemia (AML).

STING ligand-4 (Compound 2) is a nitro-free covalent STING inhibitor with an IC50 < 0.2 μM. STING ligand-4 can be used for synthesis of PROTAC STING degrader-4.

KI-ARv-03 is a potent and selective ATP-competitive CDK9 inhibitor with an IC₅₀ of 0.15 μM (at 45 μM ATP), exhibiting over 130-fold selectivity against other CDKs (including CDK1-7). KI-ARv-03 reduces androgen receptor (AR)-driven transcription and proliferation in prostate cancer cells. KI-ARv-03 can be used for leukemia, pancreatic cancer, alveolar rhabdomyosarcoma (ARMS) and castration-resistant prostate cancer (CRPC) research. KI-ARv-03 is a ligand for target protein for PROTAC. KI-ARv-03 can be used to synthesize PROTAC KI-CDK9d-32.

RET ligand-5 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC RET Degrader 1. PROTAC RET Degrader 1 is a potent RET PROTAC degrader with anti-tumor activity.

BRD2 BD1 ligand-1 is a potent BRD2 BD1 ligand (Ligands for Target Protein for PROTACs) can be used in the synthesis of PROTAC BRD2 BD1 Degrader-1.

FLT3/JAK2/BRD4 ligand-1 is a FLT3/JAK2/BRD4 ligand. FLT3/JAK2/BRD4 ligand-1 can be used for synthesis PROTAC FLT3/JAK2/BRD4 Degrader-1.

SHP2 ligand-3 is a PROTAC target protein ligand that can be used to synthesize SHP2 protein degrader-1.

ER ligand-12 is an estrogen receptor (ER) ligand that can be used in the synthesis of PROTACs, such as PROTAC ER Degrader-2.

PROTAC Her3-binding moiety 2 is a Her3 inhibitor. PROTAC Her3-binding moiety 2 can be used for synthesis of PROTAC Her3 Degrader-8.

Androgen receptor ligand 3 is an androgen receptor (AR) ligand. Androgen receptor ligand 3 is linked to an IAP ligand via a linker to form an ERα PROTAC degrader.

SARS-CoV-2 Mpro ligand 1 (Compound S15) is a PROTAC target protein ligand. SARS-CoV-2 Mpro ligand 1 can be used to synthesize BP-198.

HPK1 ligand 3 is a ligand for target protein for PROTAC that can be used to synthesize PROTAC HPK1 Degrader-4.

WZH-15-125 is a potent ALK inhibitor. WZH-15-125 can effectively overcome drug resistance, especially compound ALK mutations. WZH-15-125 has an IC50 of 101.7 nM for the highly refractory G1202R/L1196M mutation that is resistant to Lorlatinib. WZH-15-125 can be used as a PROTAC target protein ligand to synthesize PROTAC WZH-17-002. WZH-15-125 can be used in the research of non-small cell lung cancer.

ARCC-4 is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.

dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=500 nM), but is inactive on BRD4 BD2..

dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM, and has antitumor activity.

XY028-140 (MS-140) is a potent and selective PROTAC-based CDK4/CDK6 kinase degrader. XY028-140 specifically inhibits RB-E2F signaling and reduces CDK4 and CDK6 protein levels in a dose- and time-dependent manner in vitro. In addition, XY028-140 can degrade its targets by linking them with ubiquitin-proteasome mechanism. Further, the degradation of CDK4/6 protein by XY028-140 is specifically mediated by CRBN. Therefore, XY028-140 effectively and selectively inhibits and degrades CDK4/6 kinase by targeting CDK4/6 kinase in CDK4/6i-S (CDK4/6 inhibitor-sensitive) tumor cells to the CRL4-CRBN-E3 ubiquitin complex. Compared with CDK6 wild-type cells, XY028-140 treatment of cells expressing wild-type or mutation-activated CDK6 resulted in a more effective degradation of CDK6 (S178P).

KH103 is a highly potent, catalytically-driven glucocorticoid receptor (GR) PROTAC degrader, demonstrate excellent performance in passively preventing ligand-induced gene expression activation in the absence of partial agonistic transcriptional triggering and crosstalk inhibition. KH 103 efficiently degrades glucocorticoid receptor (GR) in vitro and in vivo. In HEK293 cells, KH-103 (1 µM) induced rapid and nearly complete GR degradation within one hour. This degradation was highly potent, with significant depletion observed at 10 nM and near-complete depletion at 100 nM. KH-103 demonstrated effective and ​​reversible​​ GR degradation across diverse in vitro models from multiple tissues and species.Mechanistically, KH-103 promoted GR nuclear translocation but did not activate GR-mediated gene transcription and exhibited no nonspecific transcriptional effects alone. Furthermore, KH-103 effectively blocked dexamethasone (DEX)-induced GR signaling, demonstrating greater potency than comparator inhibitors.Critically, KH-103 also effectively depleted GR protein in the mouse pituitary gland in vivo and modulated corticosterone levels, confirming pharmacological activity beyond cell-based systems.

Abd110 (compound 42i) is a PROTAC molecule derived from lenalidomide that specifically targets ATR kinase for degradation. This compound demonstrates remarkable selectivity, effectively reducing both ATR and phospho-ATR levels while sparing related DNA damage response kinases ATM and DNA-PKcs.

MS8847 represents a novel PROTAC molecule that selectively targets EZH2 for degradation by recruiting the VHL E3 ubiquitin ligase complex. This compound mediates potent, proteasome-dependent elimination of EZH2, demonstrating significant anti-proliferative effects against both AML and TNBC cell lines.