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Pathways Recommended:	Antibody-drug Conjugate/ADC Related

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Target Protein Ligand-Linker Conjugates

" in MedChemExpress (MCE) Product Catalog:

By Targets:	E3 Ligase Ligand-Linker Conjugates (2) Target Protein Ligand-Linker Conjugates (8) 17β-HSD (1) Androgen Receptor (1) Apoptosis (2) AUTACs (1) Btk (1) Casein Kinase (1) CRM1 (1) Epigenetic Reader Domain (4) Estrogen Receptor/ERR (1) FGFR (1) FKBP (1) FLT3 (1) Mitophagy (1) Molecular Glues (1) NF-κB (1) PROTACs (13) Ras (1) RET (1) SWI/SNF Complex (1)
By Research Areas:	Cancer (23) Metabolic Disease (1) Neurological Disease (1)

Targets Recommended: Target Protein Ligand-Linker Conjugates E3 Ligase Ligand-Linker Conjugates PROTAC-Linker Conjugates for PAC ADC Linker Drug-Linker Conjugates for ADC Antibody-Drug Conjugates (ADCs) Peptide-Drug Conjugates (PDCs) Radionuclide-Drug Conjugates (RDCs) PD-1/PD-L1 Ligands for Target Protein for PROTAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-132943A

BRD4 ligand-Linker Conjugate 1 TFA	Target Protein Ligand-Linker Conjugates	Cancer
BRD4 ligand-Linker Conjugate 1 TFA (compound 106-1) is a target protein ligand-linker conjugate that can be used in the synthesis of PROTACs .

HY-168693

Target Protein Ligand-Linker Conjugates 2	Target Protein Ligand-Linker Conjugates
Target Protein Ligand-Linker Conjugates 2 is a conjugate of the Target Protein Ligand and Linker, consisting of Desmethyl-QCA276 (HY-44103) and the corresponding Linker. Target Protein Ligand-Linker Conjugates 2 can be used to synthesize PROTAC BD-9136 (HY-149878) .

HY-169490

Target Protein Ligand-Linker Conjugates 4	Target Protein Ligand-Linker Conjugates	Cancer
Target Protein Ligand-Linker Conjugates 4 is a conjugate generated by linking a target protein ligand (HY-44824) to a linker (HY-169489). Target Protein Ligand-Linker Conjugates 4 can be used in the synthesis of PROTACs (e.g. PROTAC SMARCA2 degrader-21 (HY-169272)) .

HY-169488

SMARCA2 ligand-12-3-methylazetidine	Epigenetic Reader Domain Target Protein Ligand-Linker Conjugates	Cancer
SMARCA2 ligand-12-3-methylazetidin is a **target protein ligand-linker conjugate** that incorporates a ligand for SMARCA2 (HY-169487), and a PROTAC linker (HY-W052601), which recruit E3 ligases. SMARCA2 ligand-12-3-methylazetidin can be used to synthesize PROTAC SMARCA2 degrader-25 (HY-169276) .

HY-153424

PROTAC SMARCA2 degrader-1	Target Protein Ligand-Linker Conjugates	Cancer
PROTAC SMARCA2 degrader-1 (compound ex7) is a BRM2 (SMARCA2) degrader (DC₅₀<0.1 μM). PROTAC SMARCA2 degrader-1 is also an E3 ubiquitin ligase binding linker useful in research of cancers. PROTAC SMARCA2 degrader-1 is a **target protein ligand-linker conjugate** .

HY-132943

BRD4 ligand-Linker Conjugate 1	Target Protein Ligand-Linker Conjugates	Cancer
BRD4 ligand-Linker Conjugate 1 is a target protein ligand-linker conjugate that can be used in the synthesis of PROTACs.

HY-170987

FKBP12 Ligand-Linker Conjugate 1	Target Protein Ligand-Linker Conjugates FKBP	Cancer
FKBP12 Ligand-Linker Conjugate 1 is the conjugate composed of a target protein ligand for FKBP12 and a linker. FKBP12 Ligand-Linker Conjugate 1 can be used for synthesis of PROTAC degrader MC-25B (HY-170983) .

HY-169357

Acepromazine-1-Piperazinepropanamine	E3 Ligase Ligand-Linker Conjugates	Cancer
Acepromazine-1-Piperazinepropanamine (compound 10) is a synthesized E3 ligase ligand-linker conjugate (E3 Ligase Ligand-Linker Conjugate) that incorporates a cereblon ligand and a linker. Acepromazine-1-Piperazinepropanamine can be connected to the target protein ligand to form a PROTAC molecule, TrimTAC1 (HY-169355) .

HY-147225

TSPO Ligand-Linker Conjugates 1	AUTACs Mitophagy	Neurological Disease Metabolic Disease Cancer
TSPO Ligand-Linker Conjugates 1 contains a ligand for translocator protein (TSPO) and a linker, which is used for the synthesis of mitochondria-targeting autophagy-targeting chimera (AUTAC). AUTAC can bind the TSPO on the outer mitochondrial membrane (OMM) of mitochondria and degrades impaired mitochondria and proteins via mitophagy, and improves mitochondrial activity. TSPO Ligand-Linker Conjugates 1 can be used in mitochondrial dysfunction related research, including neurodegenerative diseases, cancer, and diabetes .

HY-170769

FLT3 Ligand-Linker Conjugate 1	Target Protein Ligand-Linker Conjugates FLT3	Cancer
FLT3 Ligand-Linker Conjugate 1 (compound 7) contains the FLT3 ligand and a PROTAC linker, which can recruit the E3 ligase VHL. FLT3 Ligand-Linker Conjugate 1 can be used to synthesize the PROTAC RSS0680 (HY-148062). PROTAC RSS0680 is a bifunctional compound that targets protein degradation of kinases .

HY-131886

Pomalidomide 4'-alkylC4-acid	E3 Ligase Ligand-Linker Conjugates	Cancer
Pomalidomide 4'-alkylC4-acid (linker16) is a E3 Ligase Ligand-Linker Conjugate. Pomalidomide 4'-alkylC4-acid can be used for conjugation to a target protein ligand .

HY-170332

PROTAC ER Degrader-15	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ER Degrader-15 (Compound 40) is an orally active degrader of the estrogen receptor (ER) with anticancer activity，which can be used in breast cancer research (Pink: Target Protein Ligand (HY-170334); Black: Linker (HY-30756); Blue: E3 Ligase Ligand (HY-138793); E3 Ligase Ligand-Linker Conjugate (HY-169979)) .

HY-170828

SMD-1087	PROTACs SWI/SNF Complex	Others
SMD-1087 is a PROTAC that selectively targets SMARCA2 (DC₅₀=8 nM, D_max=89%) and SMARCA4 with a DC₅₀ of 1 μM. SMD-1087 consists of the E3 ligase ligand (S,R,S)-AHPC-Me (blue part) (HY-112078), the target protein ligand SMI-1074 (red part) (HY-170817), and the PROTAC linker (1r,4r)-tert-Butyl 4-(bromomethyl)cyclohexanecarboxylate (black part) (HY-W890392). Among them, its target protein ligand + Linker part corresponds to SMARCA2 Ligand-Linker Conjugate-1 (HY-170829) .

HY-170852

QZ2135	PROTACs RET	Cancer
QZ2135 (compound 20) is a *RET*-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC₅₀ values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively. QZ2135 is composed of a target protein ligand (red part) RET ligand-3 (HY-170853), an E3 ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC Linker (black part) 7-Iodohept-1-yne (HY-W587352), in which the target protein ligand + linker form a conjugate RET Ligand-Linker Conjugate-1 (HY-170854) .

HY-170859

AH078	Casein Kinase	Others
AH078 (compound 37) is a PROTAC degrader that selectively targets CK1δ and CK1ε, and has low targeting for CK1α. AH078 consists of PROTAC linker (black part) Monomethyl octanoate (HY-W001958), target protein ligand (red part) (HY-170860) CK1δ/CK1ε liagnd-1 and E3 ligase ligand (blue part) E3 ligase Ligand 58 (HY-170861). Among them, E3 ligase ligand + linker can form a conjugate E3 Ligase Ligand-linker Conjugate 163 (HY-170862) .

HY-160221

PROTAC AR Degrader-7	PROTACs Androgen Receptor	Cancer
PROTAC AR Degrader-7 (compound 99) is a PROTAC targeting androgen receptor with an IC₅₀ value of 3 nM. PROTAC AR Degrader-7 is composed of PROTAC target protein ligand AR ligand-32 (HY-170303) (red part), E3 ligase ligand E3 ligase Ligand 44 (HY-170304) (blue part) and PROTAC Linker N-Boc-piperazine (HY-30105) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 145 (HY-170305) .

HY-142621

BCPyr	PROTACs Btk	Cancer
BCPyr is a PROTAC-class BTK degrader (DC₅₀ = 800 nM) . BCPyr consists of a PROTAC target protein ligand (red part) BTK ligand 11 (HY-168314), an E3 ubiquitin ligase ligand (blue part) E3 ligase Ligand 20 (HY-135997), and a PROTAC linker (black part) (5-(Bromomethyl)pyrazin-2-yl)methanol (HY-168315). E3 ubiquitin ligase+linker can form E3 Ligase Ligand-linker Conjugate 146 (HY-168316).

HY-168274

PROTAC TRIB2 degrader-1	PROTACs Apoptosis	Cancer
PROTAC TRIB2 degrader-1 (Compound 5k) is an effective TRIB2 degrader that selectively induces TRIB2 degradation through the CRBN-dependent ubiquitin-proteasome pathway. PROTAC TRIB2 degrader-1 can inhibit cell proliferation and induce cell apoptosis, and can be used in cancer research. (Target protein ligand (Pink): HY-168275; linker (black): HY-168276; E3 Ligase Ligand-Linker Conjugates: HY-168277; E3 ligase (Blue): HY-W023573) .

HY-170869

PROTAC FGFR1 degrader-1	PROTACs FGFR	Cancer
PROTAC FGFR1 degrader-1 (compound S2H) is a PROTAC degrader targeting FGFR1, with IC₅₀=26.81 nM and DC₅₀=39.78 nM in KG1a cells. PROTAC FGFR1 degrader-1 is composed of CRBN-type E3 ligase ligand (blue part) Pomalidomide (HY-10984), target protein ligand (red part) FGFR1 ligand-1 (HY-170871), and PROTAC linker (black part) 9-Bromononanoic acid (HY-W007587), in which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 164 (HY-170870) .

HY-157228

ACBI3	PROTACs Ras	Cancer
ACBI3 (compound 7) is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995). ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models .

HY-159651

PTOTAC HSD17B13 degrader 1	PROTACs 17β-HSD	Cancer
PTOTAC HSD17B13 degrader 1 (compound 1) is a PROTAC targeting 17β-HSD 13 (HSD17B13). PTOTAC HSD17B13 degrader 1 is composed of PROTAC target protein ligand HSD17B13 degrader 2 (HY-159662) (red part), PROTAC Linker tert-Butyl 5-bromoisoindoline-2-carboxylate (HY-W003696) (black part) and E3 ubiquitin ligase ligand E3 ligase Ligand 31 (HY-159660) (blue part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 114 (HY-159661) ^{[1] ^.}

HY-170347

PROTAC SMARCA2/4 degrader-36	PROTACs Epigenetic Reader Domain	Cancer
PROTAC SMARCA2/4 degrader-36 (Compound 29) is an effective dual degrader of SMARCA2/4,with DC₅₀ values of 0.22 nM and 0.85 nM for SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2/4 degrader-36 has anti-cell proliferation activity (Pink: Target Protein Ligand (HY-170354); Black: Linker (HY-W895794); Blue: E3 Ligase Ligand (HY-170353); E3 Ligase Ligand-Linker Conjugate (HY-170356)) .

HY-170669

PROTAC XPO1 degrader-1	PROTACs CRM1 Apoptosis NF-κB	Cancer
PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies (Pink: Target Protein Ligand (HY-170672); Black: Linker (HY-W010525); Blue: E3 Ligase Ligand (HY-170671); E3 Ligase Ligand-Linker Conjugate (HY-170673)) .

HY-145925C

(S,R)-CFT8634	PROTACs Epigenetic Reader Domain	Cancer
(S,R)-CFT8634 (compound 176) is a selective and orally active PROTAC-class BRD9 protein degrader. (S,R)-CFT8634 has the potential to study BRD9-mediated diseases, including but not limited to abnormal cell proliferation. (S,R)-CFT8634 consists of a target protein ligand (red part) BRD9 ligand-5 (HY-169988), an E3 ligase ligand (blue part) CRBN ligand-11 (HY-169989), and a PROTAC linker (black part) 1-(3,3-Difluoro-4-piperidinyl)piperazine (HY-169991). E3 ligase ligand and linker can form E3 Ligase Ligand-linker Conjugate 142 (HY-169990) .

HY-170824

SMD-3236	PROTACs Epigenetic Reader Domain	Cancer
SMD-3236 is a SMARCA2-targeted PRAOTAC degrader designed based on SMARCA ligands and VHL-1 ligands, with long-lasting antitumor activity in vivo. SMARCA2 is a synthetic lethal target in SMARCA4-deficient cancer cells, and SMD-3236 has a 2000-fold selectivity for degradation of SMARCA2 over SMARCA4, with a DC₅₀< 1 nM and a D_max>95%. SMD-3236 can induce SMARCA2 loss in tumor tissues while retaining SMARCA4 protein, and inhibit tumor growth in the H838 smarca4-deficient human cancer xenograft model. SMD-3236 is composed of target protein ligand (red part) SMI-1074 (HY-170817), PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate (HY-170825), and E3 ligase ligand (blue part) SMARCA2 ligand-14 (HY-170826), of which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 159 (HY-170827) .

HY-170820

XYD049	Molecular Glues	Cancer
XYD049 (compound 7d) is a CRBN-type molecular glue targeting GSPT1 (DC₅₀=19 nM), which can be used for the research of MYC-driven castration-resistant prostate cancer (CRPC). XYD049 can effectively inhibit the growth of 22Rv1 cells (IC₅₀=7 nM) and has in vivo antitumor efficacy. XYD049 downregulates the CRPC-related oncogenes in 22Rv1 cells, including AR, AR-v7, PSA, and c-Myc. XYD049 is composed of a molecular glue linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-type E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), in which the E3 ligase ligand + liner form a conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .

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