2. Signaling Pathways
  3. PROTAC
  4. PROTACs

PROTACs

PROTACs

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PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.

PROTACs Isoform Specific Products:

PROTACs Isoform Comparison
Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-176261
    DDD2
    DDD2 is a selective and potent VHL-mediated PROTAC NUDT5 degrader. DDD2 induces robust NUDT5 degradation. DDD2 can be used in cancer research, such as lymphocytic leukemia and osteosarcoma. (Structure Note: Pink: NUDT5 inhibitor (HY-176262); Blue: E3 (HY-125845); Black: linker (HY-W001958))
    DDD2
  • HY-178925
    PROTAC GPX4 degrader-5
    PROTAC GPX4 degrader-5 is an efficient and highly selective GPX4 PROTAC degrader (DC50 = 28 nM). PROTAC GPX4 degrader-5 can induce ferroptosis and has low toxicity to normal cells. PROTAC GPX4 degrader-5 can significantly increase ROS. PROTAC GPX4 degrader-5 exerts anti proliferative effects on various tumor cells. PROTAC GPX4 degrader-5 is commonly used in cancer research. (Pink: GPX4 Ligand (HY-179294); Blue: Hyt Hydrophobic group (HY-N2427); Black: Linker (HY-W047688))
    PROTAC GPX4 degrader-5
  • HY-162743
    PROTAC SMARCA2/4-degrader-29 2568273-82-3
    PROTAC SMARCA2/4-degrader-29 (Compound I-279) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-29 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: ligand for target protein (HY-163926); Black: linker (HY-159682); Blue: ligand for E3 ligase (HY-W382038)).
    PROTAC SMARCA2/4-degrader-29
  • HY-175354
    PROTAC BET Degrader-13
    PROTAC BET Degrader-13 (Compound 34) is a TRIM21-based PROTAC (TRIMTAC) degrader targeting BET. PROTAC BET Degrader-13 significantly degrades PML-eGFP-BRD4 fusion protein with a near-complete loss of EGFP+ nuclear puncta with an EC50 of 1.4 μM. Pink: BET ligand (HY-13030); Blue: E3 ligase ligand (HY-W1125585); Black: linker
    PROTAC BET Degrader-13
  • HY-161280
    PROTAC FLT-3 degrader 3
    PROTAC FLT-3 degrader 3 (compound 35) is a PROTACs degrader of FLT. PROTAC FLT-3 degrader 3 has antiproliferative activity, with IC50 of 7.55 nM in MV4-11 cells.
    PROTAC FLT-3 degrader 3
  • HY-174405
    PROTAC PDE4 degrader-1 3087311-36-9
    PROTAC PDE4 degrader-1 (Compound 9m) is a selective and orally active PDE4 PROTAC degrader with a DC50 of 41.98 μM. PROTAC PDE4 degrader-1 potently inhibits the secretion of pro-inflammatory cytokines such as TNF-α and IL-6. PROTAC PDE4 degrader-1 significantly alleviates pulmonary inflammation in LPS (HY-D1056)-induced acute lung injury (ALI) mice Model. Pink: PDE4 ligand (HY-174410); Blue: CRBN ligase ligand (HY-10984); Black: linker
    PROTAC PDE4 degrader-1
  • HY-178034
    PROTAC OSBP Degrader-1
    PROTAC OSBP Degrader-1 (Compound 5) is a Oxysterol-binding protein (OSBP) PROTAC degrader with a DC50 of 322 nM (24 h). PROTAC OSBP Degrader-1 can rapidly penetrate into cells and induce massive recruitment of OSBP at the Trans-Golgi network. PROTAC OSBP Degrader-1 has potent anticancer activity with potent cytotoxicity against U-87 MG, A549, MCF7, HeLa and MDA-MB-231 cells. Pink: OSBP ligand (HY-178035); Blue: CRBN ligase ligand (HY-10984); Black: linker
    PROTAC OSBP Degrader-1
  • HY-162816
    PROTAC HPK1 Degrader-3
    PROTAC HPK1 Degrader-3 (compound C3) is an orally effective PROTAC targeting HPK1 (DC50=21.26 nM). HPK1 is a negative regulator of T cell receptors, which can lead to T cell dysfunction after abnormal activation. PROTAC HPK1 Degrader-3 can inhibit SLP76 and NF-κB signaling pathways and inhibit MAPK signal transduction, and has anticancer activity and immune activation. PROTAC HPK1 Degrader-3 has a certain oral bioavailability and can be combined with PD-L1 antibody therapy to achieve a tumor growth inhibition rate of 65.58%. PROTAC HPK1 Degrader-3 is composed of E3 ligase ligand Thalidomide (HY-14658; blue part), PROTAC linker tert-Butyl 3-oxoazetidine-1-carboxylate (HY-40146; black part), and target protein ligand HPK1-IN-51 (HY-162842; red part); the activity control of the target protein ligand can be HPK1 ligand 1 (HY-162841)[1].
    PROTAC HPK1 Degrader-3
  • HY-172144
    JB300 3038446-90-8
    JB300 is a highly selective Aurora A degrader based on PROTAC technology (DC50=30 nM). JB300 can be used for tumor research. JB300 consists of PROTAC target protein ligand MK-5108 (HY-13252) (pink part), E3 ligase ligand Thalidomide-O-COOH (HY-103597) (blue part) and PROTAC Linker Boc-NH-PEG2-C2-NH2 (HY-W008474) (black part), of which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-O-COOH-NH2-C2-PEG2-NH-Boc (HY-172145).
    JB300
  • HY-159459
    PROTAC SMARCA2/4-degrader-32 2568273-79-8
    PROTAC SMARCA2/4-degrader-32 (compound I-446) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment.
    PROTAC SMARCA2/4-degrader-32
  • HY-178861
    dCDK9-202
    dCDK9-202 a potent CDK9 PROTAC degrader with an DC50 value of 3.5 nM. dCDK9-202 exhibits broad-spectrum anti-tumor activity and extensively disrupts the oncogenic transcriptome. dCDK9-202 can activate Caspase-3/7, increase the level of cleaved PARP, and directly induce apoptosis of tumor cells. dCDK9-202 effectively inhibits TC-71 tumor growth without any signs of toxicity in mice. dCDK9-202 can be used for the study of EGFR-driven cancers such as sarcoma (Pink: CDK9 ligand (HY-178862); Blue: CRBN ligand (HY-W248665); Black: Linker (HY-N8015)).
    dCDK9-202
  • HY-162544
    PROTAC HPK1 Degrader-2 2893885-31-7
    PROTAC HPK1 Degrader-2 (compound 3) is a PROTAC degrader of HPK1, with the DC50 of 23 nM in human PBMC. PROTAC HPK1 Degrader-2 plays an important role in cancer research.
    PROTAC HPK1 Degrader-2
  • HY-171859
    FC-14367 3066893-65-7
    FC-14367 is a PROTAC degrader targeting HIV-1 Nef protein. FC-14367 forms a ternary complex by binding Nef and Cereblon E3 ubiquitin ligase, inducing Nef ubiquitination and proteasomal degradation, restoring cell-surface CD4 and MHC-I expression and inhibiting HIV-1 replication. FC-14367 can be used in research on HIV infection and AIDS. (Black: Glycolic acid (HY-W015967); Blue: 2-(2,6-Dioxopiperidin-3-yl)phthalimidine (HY-138793))
    FC-14367
  • HY-156751
    (Rac)-GDC-2992 2753650-84-7
    (Rac)-GDC-2992 (Compound 1) is a PROTAC androgen receptor degrader (DC50: 10 nM in VCaP cell). (Rac)-GDC-2992 blocks the process of androgen receptor transduction and also degrades the receptor itself. (Rac)-GDC-2992 can be used for prostate cancer research. Pink: AR ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189); Black: linker (HY-169975).
    (Rac)-GDC-2992
  • HY-176871
    PROTAC SMARCA2 degrader-35 3032998-97-0
    PROTAC SMARCA2 degrader-35 (Compound 43) is a selective SMARCA2 PROTAC degrader with a DC50 < 0.1 μM for SMARCA2. PROTAC SMARCA2 degrader-35 has anticancer activity and regulates cancer cell proliferation and growth through cell cycle arrest and DNA replication inhibition in SMARCA4-deleted cancer cells. Pink: SMARCA2 ligand (HY-178414); Blue: E3 ligase ligand; Black: linker
    PROTAC SMARCA2 degrader-35
  • HY-175271
    JWJ-01-378
    JWJ-01-378 is a selective TRK PROTAC degrader. JWJ-01-378 efficiently degrades WT TRK and TPM3-TRKA fusion proteins and inhibits downstream pERK signaling, while showing limited efficacy against TRK inhibitor resistant mutants and ALK fusions. JWJ-01-378 potently suppresses cancer cell proliferation.Pink: TRK ligand (HY-160520); Blue: CRBN ligase ligand (HY-103596); Black: linker
    JWJ-01-378
  • HY-168131
    PROTAC EZH2 Degrader-3 3098718-46-5
    PROTAC EZH2 Degrader-3 (compound ZJ-20) is a EZH2 PROTAC degrader. PROTAC EZH2 Degrader-3 (5 μM, 24 h) not only potently inhibits the expression of EZH2 protein, but also had a strong inhibits effect on the expression levels of other subunits of PRC2 as well as H3k27me3 protein. PROTAC EZH2 Degrader-3 shows anti-proliferative activity and blocks the cell cycle in the G0-G1 phase and induces cell apoptosis((Blue: cereblon ligand Pomalidomide (HY-10984), Black: linker HY-W361751；Pink: EZH2 inhibitor Tazemetostat (HY-13803)).
    PROTAC EZH2 Degrader-3
  • HY-176184
    PROTAC DDR1 degrader-1 3081612-73-6
    PROTAC DDR1 degrader-1 is a PROTAC based DDR1 degrader (Red: DDR1 inhibitor (HY-176185), black: linker, Blue: E3 ligase ligand).
    PROTAC DDR1 degrader-1
  • HY-156745
    DDa-1 3036944-98-3
    DDa-1 is a potent BTK degrader (DC50: 90 nM). Blue: DCAF1 binder (HY-149934), Black: linker, Pink: BTK ligand (HY-107447).
    DDa-1
  • HY-144323
    YF135 2913177-53-2
    YF135 is an efficient and reversible-covalent KRASG12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRASG12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway.
    YF135
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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