1. Signaling Pathways
  2. PROTAC
  3. PROTACs

PROTACs

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.

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-174866
    BT-O2C 3055107-34-8
    BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines (IC50 ranges from 152 to 221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer. (Pink: p300 Ligand (HY-174868); Blue: CRBN Ligand (HY-W023573); Black: Linker; CRBN Ligand+Linker (HY-174869)).
    BT-O2C
  • HY-160151
    TP1L
    TP1L is a potent and selective T-cell protein tyrosine phosphatase (TC-PTP) PROTAC degrader, with a DC50 value of 35.8 nM. TP1L elevates the phosphorylation level of TC-PTP substrates including pSTAT1 and pJAK1. TP1L selectively enhances IFN-γ signaling and increases MHC-I expression. TP1L activates TCR signaling through increases phosphorylation of LCK. TP1L enhances CAR-T cell mediated tumor killing efficacy through activation of the CAR-T cells. TP1L can be used for the study of cancer. (Pink: TC-PTP ligand: (HY-138964), Blue: E3 ligase CRBN Ligand (HY-A0003), Black: Linker: (HY-140002)).
    TP1L
  • HY-158062
    LC-1-40
    LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). LC-1-40 selectively inhibits MYCN-induced tumor growth in mouse models. LC-1-40 also induces nucleotide damage and apoptosis in MYCN-associated tumors. LC-1-40 can be used in cancer research. (Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker).
    LC-1-40
  • HY-153674
    PROTAC SOS1 degrader-4
    PROTAC SOS1 degrader-4 (compound 10) is a potent SOS1 degrader. PROTAC SOS1 degrader-4 shows antiproliferative activity.
    PROTAC SOS1 degrader-4
  • HY-169086
    KL-465 3057446-82-6
    KL-465 is a PROTAC degrader for MAGE-A3, that degrades MAGE-A3 with a DC50 of 2 μM in HeLa cell. KL-465 inhibits viability of MAGE-A3 positive cancer cell HCT116, A375 and HeLa. (Blue: Ligand for E3 ligase (HY-151227); Black: Linker (HY-W679862); Pink: Ligand for target protein (HY-169087))
    KL-465
  • HY-163868
    PROTAC SMARCA2/4-degrader-15 2568276-81-1
    PROTAC SMARCA2/4-degrader-15 (Compound I-335) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-15 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for Target Protein (HY-159545); Black: Linker (HY-N3024); Blue: Ligand for E3 Ligase (HY-125845))
    PROTAC SMARCA2/4-degrader-15
  • HY-159461
    PROTAC SMARCA2/4-degrader-9 2568507-15-1
    PROTAC SMARCA2/4-degrader-9 (Compound I-503) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2 degrader-9 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for target protein (HY-159545); Black: Linker (HY-W006635); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2/4-degrader-9
  • HY-174210
    PROTAC BRD4 Degrader-31
    PROTAC BRD4 Degrader-31 is a BRD4 PROTAC degrader with DC50 s of 164 and 80 nM at 4 h and 24 h, respectively. PROTAC BRD4 Degrader-31 potently degrades BRD4 in cells with long acting degradation kinetics. Pink: BRD4 ligand (HY-78695); Blue: KLHDC2 ligand (HY-174218)
    PROTAC BRD4 Degrader-31
  • HY-169274
    PROTAC SMARCA2 degrader-23 2892523-67-8
    PROTAC SMARCA2 degrader-23 (Example 1) is a potent and selective PROTAC SMARCA2 degrader,with a DC50 of <100 nM. PROTAC SMARCA2 degrader-23 has the potential for the research of cancer.
    PROTAC SMARCA2 degrader-23
  • HY-138637
    PROTAC BRD4 Degrader-14 3026420-43-6
    PROTAC BRD4 Degrader-14 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.8 nM and 1.7 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-14 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
    PROTAC BRD4 Degrader-14
  • HY-170340
    PROTAC ER Degrader-14 2504911-73-1
    PROTAC ER Degrader-14 (compound 86) is a PTORAC-type Estrogen Receptor/ERR degrader, which is composed of E3 ubiquitin ligase ligand (blue part) (S)-Deoxy-thalidomide (HY-168055), PROTAC Linker (black part) N-Boc-piperazine (HY-30105) and target protein ligand (red part) ER ligand-6 (HY-170341). Among them, E3 ligase + Linker constitute tert-Butyl (S)-4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxylate (HY-W998234).
    PROTAC ER Degrader-14
  • HY-163564
    JYQ-194 98.05%
    JYQ-194 is a PROTAC degrader targeting human Parkinson's disease protein 7 (PARK7). JYQ-194 can be used in the study of cancer and neurodegenerative diseases. (Pink: PARK7 ligand (HY-163563); Black: linker (HY-W017440); Blue: E3 ligase ligand (HY-10984)).
    JYQ-194
  • HY-174315
    WZH-17-002
    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 (HY-12215)-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. Pink: ALK ligand (HY-174314); Blue: CRBN ligase ligand (HY-14658); Black: linker (HY-174316)
    WZH-17-002
  • HY-159015
    SIAIS630120-NC
    SIAIS630120-NC is a negative control for NAMPT (nicotinamide phosphoribosyltransferase) degrader SIAIS630120 (Sturcture Note:(Blue: Cereblon ligand Thalidomide (HY-14658) analogue (HY-138793), Black: linker;Pink: Nampt inhibitor FK866 (HY-50876)).
    SIAIS630120-NC
  • HY-175455
    LYA914
    LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458).
    LYA914
  • HY-170995
    PROTAC ROR1 degrader-1
    PROTAC ROR1 degrader-1 (Compound 11d) is a PROTAC degrader for pseudokinase ROR1 that degrades ROR1 in NSCLC cells with a DC50s of 40-80 nM. PROTAC ROR1 degrader-1 causes the cleavage of PARP and induces apoptosis in NCI-H23. (Pink: ligand for target protein ROR1 ligand-1 (HY-170996); Black: linker (HY-W014787); Blue: ligand for VHL E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC ROR1 degrader-1
  • HY-173561
    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((Pink: target protein ligand (HY-173562 ); Black: linker; Blue: VHL ligase (HY-47070)).
    MS115
  • HY-153425
    PROTAC SMARCA2 degrader-2 2892523-74-7
    PROTAC SMARCA2 degrader-2 is a potent and selective SMARCA2/4 PROTAC degrader with an IC50 of <0.1 μΜ in HeLa HiBiT assay. PROTAC SMARCA2 degrader-2 is extracted from patent WO2023287787A1 and has the potential for SMARCA4-related or deficient cancer research.
    PROTAC SMARCA2 degrader-2
  • HY-153414
    GXF-111
    GXF-111, a PROTAC molecule, can promote selective degradation of cellular BRD3 and BRD4-L. GXF-111 has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively. GXF-111 can be used for the research of cancer.
    GXF-111
  • HY-149963
    PROTAC CDK9 degrader-6 2935587-91-8
    PROTAC CDK9 degrader-6 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-6 mediates CDK9 degradation via the proteasome. PROTAC CDK9 degrader-6 degrades CDK9 with DC50s of 0.10 μM and 0.14 μM for the CDK942 and CDK955 isoforms, respectively.
    PROTAC CDK9 degrader-6
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