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-171334
    (Rac)-P1D-34 2957895-04-2 99.45%
    PROTAC PIN1 degrader-2 (1) is a PROTAC-based PIN1 degrader (Pink: PIN1 ligand HY-171442, Blue: cereblon ligand Thalidomide (HY-14658), Black: linker HY-W014883). PROTAC PIN1 degrader-2 (1) possesses anti-cancer activity, with IC50 values of 2248 nM (MV-4-11 cells), 3984 nM (MOLM-13), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60) and 3925 nM (HL-60) respectively.
    (Rac)-P1D-34
  • HY-147858A
    PROTAC EGFR degrader 7 diTFA 99.19%
    PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13.2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46.82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research.
    PROTAC EGFR degrader 7 diTFA
  • HY-136257
    CMP98 2244684-50-0 99.72%
    CMP98, a PROTAC, is unable to induce degradation of VHL. CMP98 can be used as a negative control compound for CM11. CMP98 consists of two von Hippel-Lindau ligands on their active domain.
    CMP98
  • HY-161233A
    BTX-6654 formate
    BTX-6654 (formate) is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 (formate) reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations.
    BTX-6654 formate
  • HY-143344
    NJH-2-056 2858812-69-6 98.23%
    NJH-2-056 is a deubiquitinase-targeting chimera (DUBTAC) linking the OTUB1 recruiter EN523 to the CFTR chaperone lumacaftor. NJH-2-056 can be used for cystic fibrosis research.
    NJH-2-056
  • HY-136688
    MI-389 2222635-92-7 99.34%
    MI-389 is a PROTAC translation termination factor GSPT1 degrader. MI-389 disrupts a target that is a shared dependency in different AML and ALL cell lines, and that MI-389 action is dependent on the CRL4CRBN E3 ligase.
    MI-389
  • HY-173679
    RBN012811 2569517-30-0 98.79%
    RBN012811 is a selectively PARP14 PROTAC degrader with a DC50 of 5 nM in KYSE-270 cells. RBN012811 significantly decreases IL-10 expression in IL-4 stimulated macrophages. Pink: PARP14 ligand (HY-150947); Blue: CRBN ligase ligand (HY-10984); Black: linker
    RBN012811
  • HY-157542
    CG428-NEG 2714560-39-9
    CG428-NEG is a TRK degrader negative control. CG428 (HY-137465) inhibits cell growth and reduce TPM3-TRKA levels.
    CG428-NEG
  • HY-111848A
    PROTAC AR Degrader-4 TFA 99.26%
    PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
    PROTAC AR Degrader-4 TFA
  • HY-132991
    ML 2-14 99.43%
    ML 2-14 is a PROTAC targeting BRD4 with a C4 alkyl linker. ML 2-14 consists of the E3 ligase ligand EN219 (HY-115715) (bule part), the target protein ligand JQ-1 (HY-13030) (red part), and the PROTAC linker (balck part). ML 2-14 can effectively degrade BRD4 in 231MFP breast cancer cells, and this effect can be reversed by the proteasome inhibitor Bortezomib (HY-10227) and the E1 activase inhibitor TAK-243 (HY-100487).
    ML 2-14
  • HY-145226
    XY-06-007 2757045-94-4 98.9%
    XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4BD1L94V degrader. XY-06-007 shows a DC50, 6 h of 10 nM against BRD4BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies.
    XY-06-007
  • HY-148381
    A947 2378056-80-3
    A947 is a potent and selective SMARCA2 proteolysis-targeting chimera molecule (PROTAC). A947 also is a potent and moderately selective SMARCA2 degrader. A947 has binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM. A947 can be used for the research of cancer.
    A947
  • HY-128838A
    (rel)-PROTAC ERRα Degrader-1 98.18%
    (rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1. PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader.
    (rel)-PROTAC ERRα Degrader-1
  • HY-161233
    BTX-6654
    BTX-6654 is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations.
    BTX-6654
  • HY-151613
    MS15 3035638-40-2
    MS15 is a potent and selective AKT PROTAC degrader. MS15 inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively.
    MS15
  • HY-111848
    PROTAC AR Degrader-4 1351169-31-7
    PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
    PROTAC AR Degrader-4
  • HY-147941
    MS9427 2772613-37-1
    MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer.
    MS9427
  • HY-138632
    PROTAC BRD4 Degrader-9 2417370-42-2 98.23%
    PROTAC BRD4 Degrader-9 (compound 8a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-9 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.86 nM and 7.6 nM, respectively.
    PROTAC BRD4 Degrader-9
  • HY-133137A
    SJF620 hydrochloride 2821938-05-8 99.28%
    SJF620 hydrochloride is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN.
    SJF620 hydrochloride
  • HY-141481
    DP-C-4 98.15%
    DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP.
    DP-C-4
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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