GDC-2992 (Compound 28A) is an orally active androgen receptor (AR) degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. GDC-2992 can be used for prostatic cancer study.

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.

Exatecan intermediate 12 is an intermediate for the synthesis of ADC toxin Exatecan. (Rac)-Fidarestat is a potent aldose reductase inhibitor.

III-31-C is a (hydroxyethyl)urea γ-secretase inhibitor. III-31-C inhibits Aऔ production with an IC50 of 10 nM in the cell-free γ-secretase assay and 200 nM in APP-transfected cells. III-31-C can be used in Alzheimer's disease research.

(9R)-RO7185876 (Compound example 16) is a γ-secretase inhibitor. (9R)-RO7185876 inhibits Αβ42 secretion. (9R)-RO7185876 can be used for the researches of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, multi-infarct dementia, dementia pugilistica or Down syndrome.

NCB-0970 is the negative control of NCB-0846. (R)-Norfluoxetine is a potent serotonin re-uptake inhibitor, with a Ki of 13 nM. (R)-Norfluoxetine can be used for the research of depression.

EXQ-2d is the inhibitor for tankyrase and inhibits TNKS1 and TNKS2 with an IC50 of 48.8 nM and 13.8 nM (pIC50=7.31 and 7.86). EXQ-2d inhibits WNT/β-catenin signaling pathway with IC50 of 515 nM. EXQ-2d exhibits anti-proliferative activity in cancer cells COLO 320DM and RKO with GI50 of 4.9 μM and 77 μM.

BMD4503-1 is a quinoxaline derivative. BMD4503-1 can inhibit the LRP5/6-Sclerostin interaction and regulate the Wnt signaling pathway.

21H7 is a selective inhibitor of the Wnt/b-catenin pathway. 21H7 markedly inhibits the growth of HFs. 21H7 potently decreases growth of breast and colon cancer cells.

1(R),2(S)-epoxy Cannabidiol (Compound 2a) is a structural analogue of phytocannabinoidsphytocannabinoids. 1(R),2(S)-epoxy Cannabidiol exhibits potent inhibitory activity against Wnt/β-catenin pathway. 1(R),2(S)-epoxy Cannabidiol is promising for research of neuroprotective agents.

GSK-3β probe-1 (10c) is a GSK-3β probe (Ex = 341 nm, Em= 574nm, ɛ= 3.51 × 104L/mol·cm−1) and can be be used in the study of Alzheimer's disease.

2-Cyanoethylalsterpaullone (compound 7) is an Alsterpaullone derivative and a PI3K/Akt signalling activator which promotes epithelium repair. Hydroxy celecoxib can be utilized in asthma research.