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-178467
    PROTAC FAK degrader 4
    PROTAC FAK degrader 4 (Compound 9C) is an efficient and selective FAK PROTAC degrader. PROTAC FAK degrader 4 has a DC50 of 3.6 nM in MDA-MB-231 cells. PROTAC FAK degrader 4 significantly inhibits tumor cell proliferation, migration, and invasion, and enhances chemotherapy sensitivity to cisplatin (HY-17394). PROTAC FAK degrader 4 can be used for research on cancer. (Pink: FAK Ligand (HY-43760); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W208616))
    PROTAC FAK degrader 4
  • HY-168236
    PROTAC SMARCA2 degrader-28 2641510-88-3
    PROTAC SMARCA2 degrader-28 (Compound 158) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 with a DC50 of 3 nM in HiBiT A549 cells. (Pink: Ligand for target protein (HY-168237); Black: Linker (HY-168238); Blue: Ligand for E3 ligase (HY-W087383))
    PROTAC SMARCA2 degrader-28
  • HY-163869
    PROTAC SMARCA2/4-degrader-16 2568273-64-1
    PROTAC SMARCA2/4-degrader-16 (compound I-337) 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-16
  • HY-163582
    PROTAC SOS1 degrader-7 3036155-26-4
    PROTAC SOS1 degrader-7 (Example 15) is a SOS1 PROTAC degrader. PROTAC SOS1 degrader-7 has anti-tumor activity . (Pink: SOS1 ligand (HY-163583); Black: linker (HY-163584); Blue: E3 ligase ligand (HY-W454906)).
    PROTAC SOS1 degrader-7
  • HY-176166
    PD-M6 3058330-82-5
    PD-M6 is an mTOR PROTAC degrader (DC50: 4.8 μM). PD-M6 promotes the ubiquitination and degradation of mTOR. PD-M6 inhibits the proliferation of HeLa, MCF-7, and HepG2 cancer cell lines (IC50 values of 11.3, 2.58, and 3.23 μM, respectively) and induces autophagy. PD-M6 specifically induces the degradation of LAMTOR1, a key protein in the mTOR signaling pathway. (Pink: target protein mTOR ligand (HY-B0795); target protein mTOR ligand activity control (HY-W150930); black: linker (HY-W008296); blue: E3 ligase CRBN ligand (HY-41547); target protein ligand activity control + linker (HY-176167)).
    PD-M6
  • HY-178242
    PROTAC EGFR degrader 16 2654821-07-3
    PROTAC EGFR degrader 16 (Compound 98) a selective EGFR PROTAC degrader with DC50 values of < 50 nM in NCI-H1975 (EGFR L858R-T970M), NCI-H3225 (EGFR L858R) and NCI-H1976 + CS (EGFR L858R-T970M-L797S). PROTAC EGFR degrader 16 can be used for the study of EGFR-driven cancerssuch as non-small cell lung cancer (Pink: EGFR ligand (HY-178313); Blue: CRBN ligand (HY-W1128702); Black: Linker; EGFR ligand + Linker (HY-178311)).
    PROTAC EGFR degrader 16
  • HY-176128
    BWA-6047
    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 (Pink: AR/AR-V7 ligand (HY-176129); Blue: E3 CRBN ligand (HY-W069604); Black: linker (HY-W069604)).
    BWA-6047
  • HY-157804
    PROTAC SARS-CoV-2 Mpro degrader-1 3029579-46-9
    PROTAC SARS-CoV-2 Mpro degrader-1 (compound 5) is a PROTAC degrader targeting the major SARS-CoV-2 protease with broad-spectrum antiviral activity.
    PROTAC SARS-CoV-2 Mpro degrader-1
  • HY-175435
    CST905 3094183-98-6
    CST905 is a potent PROTAC degrader of BRAF-V600E with a DC50 of 18 nM. CST905 is suitable for cancer research. (Structure Note: Pink: target protein ligand (HY-41747); Blue: E3 ligase ligand (HY-125845); Black: linker (HY-78378)).
    CST905
  • HY-144624
    PROTAC Axl Degrader 1
    PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 μM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis.
    PROTAC Axl Degrader 1
  • HY-155072
    PROTAC BTK Degrader-5
    PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research (Blue: E3 ligand (HY-W440230), Black: linker HY-168297;Pink:BKT inhibitor (HY-150898))1.
    PROTAC BTK Degrader-5
  • HY-177694
    PROTAC AR Degrader-11 2798907-41-0
    PROTAC AR Degrader-11 is a potent androgen receptor and androgen receptor splice variant-7 PROTAC degrader. PROTAC AR Degrader-11 shows potent cytotoxicity against both CWR22RV1 cells and VCaP cells. PROTAC AR Degrader-11 can be used in prostate cancer research. (Structure Note: Pink: Androgen Receptor ligand (HY-171809); Blue: CRBN ligand (HY-A0003); Black: linker (HY-169966))
    PROTAC AR Degrader-11
  • HY-158046
    UNC8899
    UNC8899 is a VHL-recruiting STING PROTAC degrader (DC50: 0.0.924 μM). UNC8899 can be used for viral or bacterial infection research (Blue: VHL ligand, Black: linker; Pink: STING inhibitor).
    UNC8899
  • HY-173255
    DAO-dBET1
    DAO-dBET1 is a Dual-Action-Only PROTAC containing a PROTAC degrader, dBET1 (HY-101838). DAO-dBET1 is a potent BRD4 degrader with a DC50 value of 277 nM in the presence of CoCl2. DAO-dBET1 inhibits hypoxia and Cath-L trigger with an IC50 value of 281 nM.
    DAO-dBET1
  • HY-175025
    CH091138
    CH091138 is a potent and selective KRASG12D PROTAC degrader with DC50s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRASWT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B)).
    CH091138
  • HY-162972
    PROTAC PD-L1 degrader-2 2995357-09-8
    PROTAC PD-L1 degrader-2 (Compound 9i) is a PROTAC degrader for PD-L1, that inhibits PD-L1 with an IC50 of 197.4 nM and exhibits an affinity with PD-L1 with a Kd of 301 nM. PROTAC PD-L1 degrader-2 promotes the internalization of PD-L1 on the cell membrane, and induces PD-L1 degradation via the synergistic effect of the proteasome and lysosomal pathways. PROTAC PD-L1 degrader-2 can activate the immune system, and exhibits antitumor efficacy in MC38 C57BL/6 mouse model.
    PROTAC PD-L1 degrader-2
  • HY-175417
    VHL-SNAP2-5C
    VHL-SNAP2-5C is a SNAP-fusion protein PROTAC degrader basing on a self-labeling protein SNAP tag. VHL-SNAP2-5C by endogenous tagging enables the visualization and the selective depletion of a SNAP-fusion protein, such as CLCa andEGFP. Pink: SNAP-fusion protein ligand (HY-W128709); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-Y1139)
    VHL-SNAP2-5C
  • HY-160563
    PROTAC ERα Degrader-8 3025533-68-7
    PROTAC ERα Degrader-8 (compound ii-56) is a potent PROTAC degrader of Erα, with DC50 of 0.000006 μM in MCF7 cells.
    PROTAC ERα Degrader-8
  • HY-171442
    PIN1 ligand-2 2957895-02-0
    PIN1 ligand-2 (Intermediate M6) is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PIN1 ligand-2 can be used for synthesizing PROTACT (Rac)-P1D-34 (HY-171334).
    PIN1 ligand-2
  • HY-170900
    SJ44236
    SJ44236 is the PROTAC degrader for BET that degrades BRD2 (DC50 = 0.127 nM), BRD3 and BRD4. SJ44236 exhibits cytotoxicity in cell MV4-11 and HD-MB03 with IC50s of 0.12 nM and 0.92 nM. SJ44236 downregulates the expression of c-Myc, upregulates the expression of p53. SJ44236 exhibits a good orally bioavailability of 45% in mice. (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W012935); Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 54 (HY-W890189))
    SJ44236
Cat. No. Product Name / Synonyms Application Reactivity

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