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-114404
    SJFα 2254609-27-1 99.61%
    SJFα is a 13-atom linker PROTAC based on von Hippel-Lindau ligand. SJFα degrades p38α with a DC50 of 7.16  nM, but is far less effective at degrading p38δ (DC50=299 nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5 µM.
    SJFα
  • HY-137346
    DD-03-156 2769753-69-5 99.63%
    DD-03-156 is a potent and selective degrader of CDK17 and LIMK2. The selectivity and potency of DD-03-156 is exquisite and makes an advanced starting point for the development of a chemical probe for the degradation of CDK17 (Blue: VHL ligand (HY-112078), Black: linker HY-124380 (HY-124380);Pink: BRAF inhibitor (HY-14660)).
    DD-03-156
  • HY-156568
    SMD-3040 3033109-92-8 99.91%
    SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC50: 12 nM). SMD-3040 contains SMARCA2/4 ligand, linker and VHL ligand. SMD-3040 demonstrates excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein.SMD-3040 achieves strong tumor growth inhibition in xenograft models.
    SMD-3040
  • HY-146231A
    SS47 TFA 99.88%
    SS47 TFA, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell research. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies. SS47 (TFA) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SS47 TFA
  • HY-147330B
    SJ1008030 formic
    SJ1008030 (compound 8) formic is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 formic inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 formic can be used for the research of leukemia.
    SJ1008030 formic
  • HY-161157
    dTAG-13-NEG 2451573-90-1 98.77%
    dTAG-13-NEG is a negative control of dTAG-13. dTAG-13 (HY-114421), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest.
    dTAG-13-NEG
  • HY-148061
    DB1113 2769753-53-7 99.28%
    DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades 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. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity.
    DB1113
  • HY-137344A
    dAURK-4 hydrochloride 99.44%
    dAURK-4 hydrochloride, an Alisertib (HY-10971) derivative, is a potent and selective PROTAC AURKA (Aurora A) degrader. dAURK-4 hydrochloride has anticancer effects. (Pink: Ligand for target protein (HY-10971); Black: Linker (HY-W004640); Blue: Ligand for E3 ligase Thalidomide-O-COOH (HY-103597)).
    dAURK-4 hydrochloride
  • HY-160506
    PRO-6E 2353493-69-1 99.85%
    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-153368
    Zomiradomide 2655656-99-6
    Zomiradomide is an orally active PROTAC degrader for IRAK4 (DC50=6 nM), thereby inhibiting the NF-κB signaling pathway. Zomiradomide acts also as a molecular glue, recruiting Ikaros and Aiolos, and mediating their degradation (DC50 for Ikaros is 1 nM), thereby activating the type I IFN signaling pathway. (Pink: target protein ligand PROTAC IRAK4 ligand-5 (HY-168311), Blue: E3 ligase ligand Thalidomide-4-Br (HY-W039116), Black: linker (HY-168313))
    Zomiradomide
  • HY-153459
    PROTAC BRD4 Degrader-19 2684292-71-3 98.83%
    PROTAC BRD4 Degrader-19 (compound 176) is a PROTAC that targets BRD4 protein for degradation. PROTAC BRD4 Degrader-19 can be used in cancer research.
    PROTAC BRD4 Degrader-19
  • HY-115568
    BETd-246 2140289-17-2 98.34%
    BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity.
    BETd-246
  • HY-145403
    PROTAC BRD9 Degrader-4 2633632-34-3 99.06%
    PROTAC BRD9 Degrader-4 is a BRD9 bifunctional degrader for researching cancer.
    PROTAC BRD9 Degrader-4
  • HY-111844
    PROTAC RAR Degrader-1 1351169-27-1
    PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134)).
    PROTAC RAR Degrader-1
  • HY-114324
    PROTAC PARP1 degrader 2369022-68-2 99.74%
    PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. PROTAC PARP1 degrader induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader consists of E3 ubiquitinase ligand MDM2 ligand (HY-128836), blue part; target protein ligand PAPR1 ligand (HY-171543), red part; PROTAC linker N3-PEG4-C2-NH2 (HY-128834), black part.
    PROTAC PARP1 degrader
  • HY-130714
    TD-165 2305936-56-3 99.41%
    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.
    TD-165
  • HY-147219A
    SIAIS164018 hydrochloride 99.84%
    SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857).
    SIAIS164018 hydrochloride
  • HY-139186
    PROTAC KRAS G12C degrader-1 2984236-79-3 99.15%
    PROTAC KRAS G12C degrader-1 is a Cereblon-based KRASG12C PROTAC degrader. PROTAC KRAS G12C degrader-1 induces CRBN/ KRASG12C dimerization and degrades GFP- KRASG12C in reporter cells.
    PROTAC KRAS G12C degrader-1
  • HY-137345
    DB-3-291 2769753-64-0 98.03%
    DB-3-291 is potent and selective PROTAC CSK degrader, with a Kd of 1 nM (Pink: CSK ligand (HY-131669); Blue: E3 ligase ligand (HY-103597); Black: linker (HY-N2407)).
    DB-3-291
  • HY-162250
    MS8847 3050872-59-5 99.78%
    MS8847 is a highly potent EZH2 PROTAC degrader that recruits the E3 ligase von Hippel-Lindau (VHL). MS8847 potently degrades EZH2 in a ubiquitin-proteasome system-dependent manner. MS8847 effectively inhibits the growth of acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cells.
    MS8847
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