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-139185
    PROTAC ERRα Degrader-3 2306388-65-6 98.82%
    PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.
    PROTAC ERRα Degrader-3
  • HY-149924
    CST626 3033993-13-1
    CST626 (Compound 9) is a pan-IAP degrader PROTAC. CST626 degrades XIAP, cIAP1 and cIAP2 with DC50s of 0.7, 2.4, and 6.2 nM in MM.1S cells, respectively.
    CST626
  • HY-148063
    DB0614 2769753-47-9 98.80%
    DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity.(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))
    DB0614
  • HY-133131
    PROTAC BRD4 Degrader-1 2133360-00-4 99.12%
    PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression.
    PROTAC BRD4 Degrader-1
  • HY-111593
    Homo-PROTAC pVHL30 degrader 1 2244684-49-7 99.40%
    Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC, consists of two ligands of von Hippel-Lindau.
    Homo-PROTAC pVHL30 degrader 1
  • HY-111870
    PROTAC RIPK degrader-6 2089205-64-9 99.97%
    PROTAC RIPK degrader-6 (example 1) is a Cereblon-based PROTAC targeting RIP Kinase degradation wherein the RIP2 kinase inhibitor is linked via a linker to a cereblon binder.
    PROTAC RIPK degrader-6
  • HY-141640
    MS154 2550393-21-8 99.42%
    MS154 is a first-in-class E3 ligase cereblon-recruiting EGFR degrader with Kds of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutants. MS154 potently induces the degradation of mutant but not wild-type EGFR in an E3 ligase-dependent manner in cancer cell lines. MS154 potently inhibits cell proliferation in lung cancer cells (Blue: E3 Ligase ligand (HY-103596); Black: linker (HY-W096167); Pink: EGFR ligand (HY-168305)).
    MS154
  • HY-135345
    PROTAC FKBP Degrader-3 2079056-43-0 99.48%
    PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader.
    PROTAC FKBP Degrader-3
  • HY-149209
    LL-K8-22 99.76%
    LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research. (Pink: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) .
    LL-K8-22
  • HY-151613A
    MS15 TFA 99.86%
    MS15 TFA is a potent and selective AKT PROTAC degrader. MS15 TFA inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively.
    MS15 TFA
  • HY-123911
    dBET23 1957234-83-1
    dBET23 is a highly effective and selective PROTAC BRD4 degrader with a DC50/5h of ~ 50 nM for BRD4BD1 protein.
    dBET23
  • HY-162608
    PROTAC JAK1 degrader 1 3052553-20-2 99.97%
    PROTAC JAK1 degrader 1 degrader 1 (compound 10c) is an effective and selective PROTAC JAK1 degrader with a DC50 of 214 nM. PROTAC JAK1 degrader 1 has antitumor activity. (Structure Note: PINK, JAK1 ligand 1 (HY-10961); Blue, VHL ligand Thalidomide (HY-14658); Black, linker).
    PROTAC JAK1 degrader 1
  • HY-137343
    DB-0646 2769753-59-3 ≥98.0%
    DB-0646, a PROTAC, is a multi-kinase degrader.
    DB-0646
  • HY-163897
    PROTAC NCOA4 degrader-1 99.42%
    PROTAC NCOA4 degrader-1 (Compound V3) is a PROTAC NCOA4 degrader (DC50: 3 nM in HeLa cells). PROTAC NCOA4 degrader-1 is a ferroptosis inhibitor. PROTAC NCOA4 degrader-1 reduces NCOA4 levels and downregulates intracellular ferrous iron (Fe2+) levels. PROTAC NCOA4 degrader-1 ameliorates liver damage in a CCl4-induced acute liver injury model. (Red: NCOA4 ligand (HY-149457). Black: linker (HY-163903). Blue: VHL ligand (HY-138678B)).
    PROTAC NCOA4 degrader-1
  • HY-148290
    KTX-951 2573298-36-7 98.03%
    KTX-951 is an orally active IRAK4 and IMiD (Ikaros/Aiolos) substrates PROTAC degrader. KTX-951 has DC50 of 13 nM, 14 nM and 13 nM for IRAK4, Ikaros and Aiolos, respectively. TX-951 has antitumor activity.(Pink: IRAK4 ligand-12 (HY-48932); Black: Linker (HY-W382009); Blue: CRBN Ligand Pomalidomide (HY-10984))
    KTX-951
  • HY-139682A
    Dovitinib-RIBOTAC TFA 2759351-69-2 98.97%
    Dovitinib RIBOTAC TFA is an RNA-targeting RIBOTAC degrader that can specifically bind to and degrade pre-miR-21. Dovitinib RIBOTAC TFA can inhibit the metastasis of breast cancer and has anti-tumor activity.
    Dovitinib-RIBOTAC TFA
  • HY-101460
    Tz-Thalidomide 2087490-42-2 98.01%
    Tz-Thalidomide is a tetrazine tagged Thalidomide (HY-14658) (Ligands for E3 Ligase). Tz-Thalidomide has binding affinity for BRD4, with IC50s of 46.25 μM (BRD4-1) and 62.55 μM (BRD4-2). Tz-Thalidomide is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.
    Tz-Thalidomide
  • HY-103633
    PROTAC BET Degrader-1 2093386-22-0 99.41%
    PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
    PROTAC BET Degrader-1
  • HY-153357
    NRX-0492 2416130-57-7 98.16%
    NRX-0492 is an orally active PROTAC-class BTK degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC50 ≤ 0.2 nM, DC90 ≤ 0.5 nM). NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 can bind non-covalently to the BTK binding domain and cereblon, which is an adapter protein in the E3 ubiquitin ligase complex. NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263). E3 ubiquitin ligase and linker can form Thalidomide 5-pyrrolidine-CHO (HY-49372A); the active control for the target protein ligand is BTK ligand 12 (HY-49421).
    NRX-0492
  • HY-112718
    PROTAC BET Degrader-10 1957234-97-7 98.23%
    PROTAC BET Degrader-10 is a potent BET protein BRD4 degrader extracted from patent WO2017007612A1, example 37, connected by ligands for Cereblon and BRD4, with a DC50 of 49 nM.
    PROTAC BET Degrader-10
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