Thalidomide-PEG2-CH2-Boc-acid is a synthesized E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs, such as MT-802.

MI1013 is a PROTAC PXR degrader (DC50 = 89 nM, Dmax = 82%). MI1013 degrades PXR in human hepatocellular carcinoma RG cells (HepaRG). MI1013 specifically and safely regulates CYP3A4 promoter activity through PXR degradation. MI1013 affects several key genes involved in sulfate conjugation (e.g., SULT1E1), bile acid synthesis (CYP7A1), gluconeogenesis (PCK1), ketone synthesis (HMGCS20), and hepatocyte proliferation (MKI67).

JP-163-16 is a RelA/p65 PROTAC degrader. JP-163-16 selectively reduces the expression of RelA/p65 in a proteasome-dependent manner in cells. JP-163-16 can induce cell apoptosis by inhibiting the NF-κB signaling pathway. JP-163-16 can be used for research on RelA/p65-dependent tumours, such as chronic lymphocytic leukaemia (CLL).

PRMT5 ligand 2 (Compound 38) is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PRMT5 ligand 2 can be used for synthesis MS115.

MS115 is a selective PRMT5/MEP50 PROTAC degrader with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and PRMT5 at 24 h in MDAMB468 cells, respectively. MS115 inhibits the proliferation of breast cancer cells.

Piperazine-CO-C1-Azacyclohexane-C1-Piperazine is a PROTAC linker can be used in the synthesis of PROTACs, such as PROTAC CDK4/6/9 degrader 1.

CPS-021 is a selective PAK4 PROTAC degrader with a DC50 of 50 nM. CPS-021 has potent antimigratory and invasive activity and significantly suppresses the invasion and metastasis of tumor cells in A549-luc lung metastasis mice model. Pink: PAK4 ligand.

ZSH-2117 is a covalent and selective EGFR PROTAC degrader with a DC50 of 45 nM in Ba/F3-EGFRL858R/T790M/C797S cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFRL858R/T790M/C797S xenograft mice model.

NASA-linker-VH032-PEG3 ligand is a ligand that can be used to synthesize PROTACs.

N-Demethylonalespib is a ligand for E3 ligase. N-Demethylonalespib can be used for synthesis of DDO3602.

Thalidomide-N-C-piperidine-C7-Br, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and a linker. Thalidomide-N-C-piperidine-C7-Br can be used in the synthesis of ZS3-046.

SK2187 is a selective AURKA PROTAC degrader with a DC50 of about 10 nM. SK2187 exhibits growth inhibition against NGP cells with an IC50 of 101.5 nM. SK2187 can be used for the study of MYCN-amplified neuroblastoma.

Thalidomide-piperidine-azetidine-Br is an E3 ligase ligand-linker conjugate that incorporates the Thalidomide based CRBN ligand and linker. Thalidomide-piperidine-azetidine-Br can be used for synthesis of BY13.

DBCO-PEG9-amine (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. DBCO-PEG9-amine (TFA) is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.

BTK ligand 11-alcohol-PEG6-azido is a synthesized E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs, such as TDP-43 degrader-1.

Dihydrouracil-Ph-2-Me-piperidine is an E3 ligase ligand. Dihydrouracil-Ph-2-Me-piperidine can be used to synthesize PROTAC HPK1 Degrader-6.

JQ1-S(GlcNAc)Cq is a sugar-coated BRD4 PROTAC degrader. JQ1-S(GlcNAc)Cq can inhibit the formation of the ternary complex between CRBN and BRD4(BD1/BD2). JQ1-S(GlcNAc)Cq can be used for the research of cancer.

(S,R,S)-AHPC-Me-amide-C15-acid is a synthesized E3 ligase ligand-linker conjugate that can be used for synthesis of PROTACs such as C199.

C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity.

PFI-7-O-C4-piperazin is a E3 ligase ligand-linker conjugate that can be used for synthesis of PROTACs, such as NEP162. The E3 ligase ligand (PFI-7) of NEP162 is a highly selective antagonist of GID4 (KD = 0.22 μM). NEP162 is a BRD4 PROTAC degrader with anti-tumor activity[1].

NEP162 is a BRD4 PROTAC degrader with DC50s of 1.2 and 1.6 μM in SW480 and U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibits tumor growth and induces apoptosis. NEP162 can be used for the study of osteosarcoma, colorectal cancer and non-small cell lung cancer, etc.

Boc-4-(3-oxobutyl)piperidine-(S,R,S)-AHPC is an E3 ligase ligand-linker conjugatecan be used in the synthesis of PROTAC BRD2 BD1 Degrader-1.

XIAP ligand-Linker Conjugate 1 is an E3 ligase ligand-linker conjugate that incorporates the XIAP BIR2 ligand XB2M54 and linker. XIAP ligand-Linker Conjugate 1 can be used for synthesis of PROTAC ERα Degrader-1.

HPK1 ligand 4 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC HPK1 Degrader-5. PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader with anti-tumor activity.

F3-PEG8-RiboTAC is a RiboTAC that can specifically degrade the mRNA of the oncogene LGALS1. F3-PEG8-RiboTAC can induce tumor cell apoptosis and inhibit invasion. F3-PEG8-RiboTAC has anti-tumor activity and can be used in the research of tumors such as leukemia and triple-negative breast cancer.

WZH-17-002 is a WZH-15-125-based ALK PROTAC degrader with a DC50 of 25 nM. WZH-17-002 enhances activities against Lorlatinib-resistant ALK compound mutations. WZH-17-002 significantly reduces drug resistance in ALK-fusion non-small cell lung cancer (NSCLC) and inhibits tumor growth in EML4-ALK G1202R/L1196 M xenograft mice model.

Thalidomide (methylamino)acetaldehyde is an E3 ubiquitinase ligand-linker conjugate. Thalidomide (methylamino)acetaldehyde can be used to synthesize WZH-17-002.

E3 Ligase Ligand-linker Conjugate 212 is a PROTAC E3 ligase-linker conjugate that can be used for synthesis of PROTACs, such as PROTAC IKZF1/3 Degrader-1. PROTAC IKZF1/3 Degrader-1 is a potent IKZF1/3 PROTAC degrader with neuroprotective activity.

NH2-PEG-phenol-PEG-COOtBu is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs, such as PROTAC BRD4 Degrader-14.

Nef ligand-2 is a binder of Nef. Nef ligand-2 is Ligands for E3 Ligase. Nef ligand-2 is the Nef Binder portion of FC-14369.