1. Signaling Pathways
  3. PROTACs
  4. PROTACs Inhibitor

PROTACs Inhibitor

PROTACs Inhibitors (22):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-112588
    dBET6 1950634-92-0 99.73%
    dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity.
  • HY-114312
    MD-224 2136247-12-4 98.08%
    MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.
  • HY-130709
    PROTAC CDK2/9 Degrader-1 2408641-24-5 99.85%
    PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand.
    PROTAC CDK2/9 Degrader-1
  • HY-130602
    MS432 2672512-44-4 98.20%
    MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.
  • HY-130257
    CP5V 2509359-75-3 98.06%
    CP5V is a PROTAC connected by ligands for von Hippel-Lindau and CDK, which specifically degrades Cdc20 by linking Cdc20 to the VHL/VBC complex for ubiquitination followed by proteasomal degradation. CP5V induces mitotic inhibition and suppresses cancer cell proliferation.
  • HY-125834
    GMB-475 2490599-18-1 99.20%
    GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
  • HY-141438
    SIM1 2719051-84-8 99.72%
    SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity.
  • HY-130714
    TD-165 2305936-56-3 98.01%
    TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group.
  • HY-115997
    PROTAC HSP90 degrader BP3 2669072-88-0 98.56%
    PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 µM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell.
    PROTAC HSP90 degrader BP3
  • HY-123919
    TL13-112 2229037-19-6
    TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib (HY-15656) and the Cereblon ligand of Pomalidomide (HY-10984).
  • HY-122582
    TL13-12 2229037-04-9 98.06%
    TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the Cereblon ligand of Pomalidomide (HY-10984).
  • HY-130256
    β-NF-JQ1 2380000-55-3
    β-NF-JQ1 is a PROTAC that recruits Aryl Hydrocarbon Receptor E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity.
  • HY-135558
    PROTAC BRD4 Degrader-3 2313234-00-1
    PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC connected by ligands for von Hippel-Lindau and BRD4.
    PROTAC BRD4 Degrader-3
  • HY-145947
    PROTAC BRD9 Degrader-5 2704616-86-2
    PROTAC BRD9 Degrader-5 is a PROTAC for targeted degradation of BRD9.
    PROTAC BRD9 Degrader-5
  • HY-135382A
    PROTAC IRAK4 degrader-3 2374122-43-5
    PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau.
    PROTAC IRAK4 degrader-3
  • HY-144323
    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.
  • HY-139315
    PROTAC IRAK4 degrader-4 2360528-45-4
    PROTAC IRAK4 degrader-4 is a Cereblon-based PROTAC as interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-127.
    PROTAC IRAK4 degrader-4
  • HY-146346
    HD-TAC7 is a potent PROTAC HDAC degrader with IC50 values of 3.6 μM, 4.2 μM and 1.1 μM for HDAC1, HDAC2 and HDAC3, respectively. HD-TAC7 can decreases NF-κB p65 in RAW 264.7 macrophages. HD-TAC7 can be used for the research of inflammatory diseases like asthma and chronic obstructive pulmonary disease (COPD).
  • HY-144657
    PROTAC SOS1 degrader-2
    PROTAC SOS1 degrader-2 is a potent PROTAC SOS1 degrader. PROTAC SOS1 degrader-2 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. PROTAC SOS1 degrader-2 significantly inhibits the tumor growth in vivo.
    PROTAC SOS1 degrader-2
  • HY-147330
    SJ1008030 (compound 8) is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 inhibits MHH–CALL-4 cells with an EC50 of 5.4 nM and an IC50 of 32.09 nM. SJ1008030 can be used for the research of leukemia.