FKBP12 PROTAC FM4 is a PROTAC degrader of MTH1, with a DC50 values of 0.09–0.22 nM.

FF2049 is a selective HDAC PROTAC degrader (DC50 = 257 nM for HDAC1). FF2049 promotes ubiquitination and degradation of HDAC. FF2049 promotes Apoptosis. FF2049 can be used for the research of hematological and solid cancer.

FDU73 is a highly effective and selective BTK PROTAC degrader with a DC50 of 2.9 nM (in JeKo-1 cells). FDU73 can inhibit the proliferation of tumor cells and exhibits anti-tumor activity.

F1-RIBOTAC is a ribonuclease-targeting chimeras (RIBOTACs). F1-RIBOTAC decreases QSOX1-a mRNA expression level in an RNase L-dependent manner. F1-RIBOTAC can be used for the research of cancer.

ERD-12310A is a PROTAC targeting Estrogen Receptor α (ERα) with a ED50 value of 47 pM. ERD-12310A has oral activity.

DU-14 (PTP1B/TC-PTP PROTAC) is a potent and selective PTP1B and TC-PTP dual PROTAC degrader. DU-14 (PTP1B/TC-PTP PROTAC) has the IC50 for PTP1B and TC-PTP phosphatase activity of 24.2 nM and 30.1 nM, respectively. DU-14 (PTP1B/TC-PTP PROTAC) enhances IFN-γ signaling, promotes T cell activation, and has anti-tumor activity.

DP-15 is the degrader for GSPT1 and BRD4 with DC50s of 5.25 nM and 0.48 nM. DP-15 exhibits anti-proliferative activity of AML cells and NHL cells with an IC50 of nanomolar levels, arrests the cell cycle at G1 phase, and induces apoptosis in MOLM13. DP-15 exhibits anti-leukemia activity in MOLM-13 xenograft mouse models.

dBAZ2B is a BAZ2B PROTAC degrader, with a DC50 of 19 nM.

dBAZ2 is a first-in-class BAZ2A and BAZ2B PROTAC degrader with DC50 values of 180 nM and 250 nM for BAZ2A and BAZ2B, respectively.

DAO-dBET1 is a Dual-Action-Only PROTAC containing a PROTAC degrader, dBET1.

CW-2 is a PARP1 PROTAC degrader. CW-2 has potent antiproliferative effects against MDA-MB-231 cells (IC50 = 0.72 μM) and CDDP-resistant cells (A549/CDDP: IC50 = 3.52 μM). CW-2 has synergistic antitumor activity and enhanced membrane permeability. CW-2 exerts antitumor effects by inducing DNA damage, impairing DNA repair, and activating mitochondria-dependent apoptosis.

BWA-6047 is a dual AR/AR-V7 and GSPT1 PROTAC degrader (AR: DC50 = 3.7 nM; AR-V7: DC50 = 3.0 nM; GSPT1: DC50 = 1.2 nM). BWA-6047 promotes ubiquitination and degradation of AR/AR-V7 and, through its molecular glue properties, induces the formation of a PPI between GSPT1 and CRBN, leading to GSPT1 degradation. BWA-6047 can be used in prostate cancer research.

BTR2004 is a selective BET family (BRD2/3/4) protein PROTAC degrader. BTR2004 forms a ternary complex with BRD proteins and KLHL20, inducing ubiquitination and proteasomal degradation through the UPS pathway. BTR2004 is promising for research of PC3 prostate cancer and MDA-MB-231 breast cancer cell lines.

AP-1 is a PROTAC targeting anaplastic lymphoma kinase (ALK). AP-1 is composed of PROTAC target protein ligand CS-1243648, E3 ligase ligand Pomalidomide and PROTAC Linker 2-(Tert-Butoxy)-2-oxoacetic acid.

AB3067 is a PROTAC degrader for BET protein, that recruits two different E3 ligase Cereblon and VHL with good affinity (IC50=559 nM for VHL in live HEK293; IC50=190 nM for CRBN in live HEK293), and degrades BRD2, BRD3, BRD4 and CRBN with DC50 of 2.1~2.3, 1.6, 15 and 75 nM, respectively. AB3067 inhibits the proliferation of RKO cell with an EC50 of 111 nM.

AA-BR-157 is a PROTAC degrader for metallothionein 2A (MT2A) with a DC50 of 190 nM. AA-BR-157 downregulates the cytoskeleton and cell motility regulating protein DIAPH3, inhibits the migration of MDA-MB-231 and U-87 MG. AA-BR-157 regulates the zinc homeostasis in MDA-MB-231.

10-SLF is a PROTAC FKBP12 degrader. 10-SLF induces a ternary complex between FKBP12 and FBXW7-R465C, and promotes FBXW7-R465C-dependent proteasomal degradation of FKBP12. 10-SLF selectively reduces FKBP12 levels in cells expressing FBXW7-R465C.

(S)-dHTC1 is a molecular glue degrader targeting the transcriptional co-activator ENL. (S)-dHTC1 binds the ligase with high affinity only after forming the ENL:dHTC1 complex with an IC50 value of 93 nM. (S)-dHTC1 degrades ENL in MV4;11 cells with a DC50 value of 26 nM. (S)-dHTC1 can be used for acute myeloid leukemia study.

PROTAC PIN1 degrader-2 is a PROTAC-based PIN1 degrader. PROTAC PIN1 degrader-2 possesses anti-cancer activity, with IC50 values of 2248 nM (MV-4-11 cells), 3984 nM (MOLM-13), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60) and 3925 nM (HL-60) respectively.

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.

THAL-SNS-032 is a novel CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).

HJM-561 is a potent, selective and orally bioavailable EGFR PROTAC degrader, selectively degrades the EGFR C797S-containing triple mutants Del19/T790M/C797S and L858R/T790M/C797S with DC50 values of 9.2 nM and 5.8 nM, respectively.

KT-253 is a potent small molecule that stabilizes p53 while simultaneously acting as a PROTAC to degrade MDM2 (DC50 = 0.4 nM). It demonstrates strong antiproliferative effects in RS4;11 leukemia cells (IC50 = 0.3 nM), inducing G2/M cell cycle arrest and apoptosis. In vivo studies confirm its antitumor activity in mouse models.

KT-333 is a first-in-class molecular glue that induces ​selective degradation of STAT3 via the ubiquitin-proteasome system by simultaneously engaging ​STAT3 and the VHL E3 ligase. This novel mechanism enables potent ​STAT3 depletion with minimal off-target effects, demonstrating strong ​anti-tumor activity in hematologic malignancies.

BTK-IN-29 (compound 14) is an inhibitor of Btk.

PROTAC BRD4 Degrader-21 (Compound 74) is a potent and selective degrader of BRD4, demonstrating robust tumor growth suppression in mouse xenograft models. Its efficacy supports its potential as a promising candidate for anticancer drug development.

SD-436 is a highly potent and selective STAT3 degrader with DC50 of 0.1 nM in human PBMCs and displays >10,000-fold degradation selectivity for STAT3 over other STAT proteins.

SD-36 (STAT3 degrader SD-36) is a potent, selective STAT3 degrader (PROTAC), potently induces the degradation of STAT3 protein in vitro and in vivo.SD-36 is designed using an analogue of CRBN ligand lenalidomide and the STAT3 inhibitor SI-109, binds to recombinant STAT3 protein with Ki of 11 nM.SD-36 (250 nM) depleted >90% of STAT3 protein in MOLM-16 cells after 4 hr treatment and >50% of STAT3 protein in DEL, KI-JK and SU-DHL-1 cells after 7 hr treatment, also efficiently degraded STAT3 protein in murine cells.SD-36 displays extremely high cellular selectivity for degradation of STAT3 over other STATs.SD-36 effectively degrades both wild-type and mutated STAT3 proteins in cells, effectively degrades mutated STAT3 (D661Y, K658R mutant), also effectively degrades CRISPR-mutated homozygous Y705F mutant STAT3 protein in DLD-1/STAT3Y705F/Y705F cells.SD-36 displayed strong growth-inhibitory activities in a subset of leukemia and lymphoma cell lines (MOLM-16 cell line IC50, 35 nM), 100-fold more potent than SI-109.SD-36 (i.v. 25 mg/kg) effectively and selectively depletes STAT3 protein, achieves complete and long-lasting tumor regression in in mouse xenograft tumors.