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-163144
    DAS-5-oCRBN 3044084-97-8 98.75%
    DAS-5-oCRBN is a selective and potent PROTAC degrader of c-Src kinase. DAS-5-oCRBN has antiproliferative activity in both c-Src-dependent cell lines.
    DAS-5-oCRBN
  • HY-150259
    MDEG-541 98.05%
    MDEG-541 is a potent MYC-MAX degrader. MDEG-541 is a PROTAC that based on the MYC-MAX dimerization inhibitor 10058-F4 derivative 28RH and Thalidomide (HY-14658). MDEG-541 shows antiproliferative activity. MDEG-541 decreases the expression of GSPT1, MYC, GSPT2, PLK1 protein.
    MDEG-541
  • HY-122822
    GSK699 2260944-68-9 98.80%
    GSK699 is a KAT2A/B/PCAF/GCN5 PROTAC degrader. GSK699 induces proteasome-dependent degradation of KAT2A, KAT2B, PCAF and GCN5, regulates the histone acetyltransferase activity of the SAGA complex, and reduces the level of histone H3K9ac. GSK699 inhibits the growth of neuroblastoma, acute myeloid leukemia and small cell lung cancer cells. GSK699 reduces the production of inflammatory cytokines and chemokines, and impairs LPS-stimulated immune cell responses. GSK699 is applicable to research related to acute myeloid leukemia, small cell lung cancer, neuroblastoma and inflammatory diseases.
    GSK699
  • HY-152227
    PROTAC TYK2 degradation agent1 2921556-14-9 99.50%
    PROTAC TYK2 degradation agent1 is a potent and subtype-selective TYK2 degrader. PROTAC TYK2 degradation agent1 has TYK2 degradation activity with DC50 value of 14 nM. PROTAC TYK2 degradation agent1 can be used for the research of autoimmune disease.
    PROTAC TYK2 degradation agent1
  • HY-111758
    PROTAC B-Raf degrader 1 2364367-27-9 99.78%
    PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.
    PROTAC B-Raf degrader 1
  • HY-145282
    MS170 2376136-61-5 98.68%
    MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC50 value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with Kds of 1.3 nM, 77 nM, and 6.5 nM, respectively.
    MS170
  • HY-136250A
    BSJ-03-204 triTFA 99.87%
    BSJ-03-204 triTFA is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 triTFA is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 triTFA does not induce IKZF1/3 degradation and has anti-cancer activity.
    BSJ-03-204 triTFA
  • HY-139436
    ARD-2585 2757422-79-8 98.19%
    ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
    ARD-2585
  • HY-169360
    SD-436 2497585-50-7 98.27%
    SD-436 is a highly selective and efficacious STAT3 PROTAC degrader (DC50: 0.5 μM), with IC50 of 19 nM (STAT3), 270 nM (STAT1), 360 nM (STAT4), >10 μM (STAT5) and >10 μM (STAT6). SD-436 promotes ubiquitination and degradation of STAT3, and induces tumor regression. SD-436 can be used for tumor research, such as leukemia and lymphoma (Pink: STAT3 ligand (HY-169361); Blue: E3 ligase ligand (HY-43722); Black: linker (HY-147052).
    SD-436
  • 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-148065
    FMF-06-098-1 2769753-07-1 98.77%
    FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1.
    FMF-06-098-1
  • HY-168593
    PROTAC KDM3 degrader-1 3119090-33-1 99.07%
    PROTAC KDM3 degrader-1 (Compound 4) is a CRBN-recruiting PROTAC designed based on the IOX1 (HY-12304) scaffold. PROTAC KDM3 degrader-1 selectively degrades the KDM3A and KDM3B proteins, thereby inhibiting the Wnt/β-catenin signaling pathway. PROTAC KDM3 degrader-1 significantly suppresses the self-renewal capacity of colorectal cancer stem cells and inhibits the growth of colorectal cancer tumors. PROTAC KDM3 degrader-1 is suitable for research on colorectal cancer (Target protein ligand (Pink): HY-12304; linker (Black): HY-22335; Conjugate of E3 ligase ligand and linker: HY-112599; E3 ligase (Blue): HY-41547).
    PROTAC KDM3 degrader-1
  • HY-149843
    LC-MB12 2828438-38-4 98.10%
    LC-MB12 is an orally active PROTAC compound targets FGFR2 degradation with a DC50 of 11.8 nM. LC-MB12 contains BGJ398 (a FGFR2 inhibitor), PROTAC linker and CRBN.LC-MB12 inhibits FGFR2 signaling in gastric cancer cells and has anti-tumor activity.
    LC-MB12
  • HY-158142
    PROTAC TYK2 degrader-1 2770470-20-5 99.55%
    PROTAC TYK2 degrader-1 (CPD-155) is a PROTAC targeting degrader to TYK2 with Dmax >60%.
    PROTAC TYK2 degrader-1
  • HY-160506
    PRO-6E 2353493-69-1 99.10%
    PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker;Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)).
    PRO-6E
  • HY-112557
    PROTAC TBK1 degrader-2 2052306-13-3 98.20%
    PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM).
    PROTAC TBK1 degrader-2
  • HY-171770
    dAurAB5 3115765-45-9 99.03%
    dAurAB5 is a dual Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM) PROTAC degrader. dAurAB5 induces degradation of Aurora-A and Aurora-B, reduces N-Myc levels, and decreases viability in IMR32 neuroblastoma cells. dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. dAurAB5 can be used to study cancers such as neuroblastoma. (Pink: TTK ligand 2: HY-168542, Blue: Thalidomide-O-COOH: HY-103597, Black: 6-Aminocaproic acid: HY-B0236).
    dAurAB5
  • HY-171767
    SK2188 3038446-94-2 99.87%
    SK2188 is a highly efficient and selective PROTAC degrader targeting AURKA (DC50 = 3.9 nM). SK2188 induces DNA damage and cell apoptosis. SK2188 indirectly degrades MYCN, inhibits tumor cell proliferation, and provides insights into the study of MYCN-amplified neuroblastoma (Pink: AURKA ligand: MK-5108 (HY-13252); Blue: Thalidomide (HY-14658); Black: Linker: Amino-PEG4-alcohol (HY-W008005)).
    SK2188
  • HY-131865
    SJF-1521 2230821-40-4 99.65%
    SJF-1521 is a selective EGFR PROTAC degrader. SJF-1521 is capable of inducing EGFR degradation in OVCAR8 cells. SJF-1521 can be used for tumor research. (Pink: EGFR ligand (HY-177379); Black: Linker (HY-128804); Blue: VHL Ligand (HY-125845)).
    SJF-1521
  • HY-156744
    DBr-1 98.87%
    DBr-1 is a potent BRD9 PROTAC degrader (KD: 13 nM). DBr-1 can overcome intrinsic resistance to VHL-degrader. Blue: DCAF1 binder (HY-149934), Black: linker, Pink: BRD9/BRD7 bromodomains inhibitor (HY-100352).
    DBr-1
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