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-128842
    PROTAC MDM2 Degrader-3 2249750-23-8
    PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
    PROTAC MDM2 Degrader-3
  • HY-139309
    PROTAC Bcl-xL degrader-2 2920415-08-1 98.23%
    PROTAC Bcl-xL degrader-2 is a potent Bcl-xL (Bcl-2 family member) degrader based on von Hippel-Lindau ligand, with an IC50 of 0.6 nM.
    PROTAC Bcl-xL degrader-2
  • HY-114402
    ARD-69 2316837-10-0 99.61%
    ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study the treatment of castration-resistant prostate cancer (mCRPC).
    ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).
    ARD-69
  • HY-169093
    MS41 2768610-97-3
    MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), respectively. MS41 effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest and increases apoptosis. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression. Red: ENL ligand (HY-169094). Black: linker (HY-W105744). Blue: VHL ligand (HY-112078).
    MS41
  • HY-160469
    INY-05-040 2503018-29-7 98.67%
    INY-05-040 is an AKT degrader that can selectively and quickly degrade all three AKT isoforms. INY-05-040 exhibits anti-cancer activity. INY-05-040 can inhibit downstream signaling and cell proliferation in 288 cancer cell lines. INY-05-040 can suppress AKT signaling and induces the stress mitogen-activated protein kinase (MAPK) c-Jun N-terminal kinase (JNK). INY-05-040 is effective for breast cancer lines with a low-baseline activation of stress MAPK pathway. INY-05-040 can be studied for anti-cancer research.
    INY-05-040
  • HY-132857A
    ZXH-4-130 TFA 2711006-67-4 99.71%
    ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC). ZXH-4-130 TFA induces ~80% CRBN degradation at 10 nM in MM1.S cells.
    ZXH-4-130 TFA
  • HY-156568B
    SMD-3040 formate 99.78%
    SMD-3040 formate is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 formate can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 formate can be used in the study of tumors such as melanoma. (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))
    SMD-3040 formate
  • 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-156366
    SNX7886 2924557-42-4 99.97%
    SNX7886 is a potent protac degrader of CDK8/19. SNX7886 degrades CDK 8 and CDK 19 with 90% and 80% degradation in 293 cells, respectively.
    SNX7886
  • HY-164233
    YX968 2742732-92-7 98.06%
    YX968 is a potent and selective HDAC3/8 PROTAC dual degrader with DC50 values of 1.7 and 6.8 nM. YX968 exhibits antitumor activity by promoting apoptosis.(Pink: Target protein ligand (HY-168287); Black: linker (HY-W007700); Blue: E3 ligase ligand (HY-112078))
    YX968
  • HY-P10899
    ETTAC-2 98.22%
    ETTAC-2 is a LRG1 PROTAC degrader. ETTAC-2 promotes ubiquitination and degradation of LRG1 (DC50 of 8.38 µM). ETTAC-2 inhibits the TGF-β-Smad3 signaling pathway and diminishes the secretion of fibrosis-associated proteins. ETTAC-2 attenuates the progression of renal fibrosis.
    ETTAC-2
  • HY-156591
    PROTAC MLKL Degrader-1 3032600-90-8 99.76%
    PROTAC MLKL Degrader-1 (Compound 36) is a PROTAC degrader of MLKL, with a Dmax ＞90%. PROTAC MLKL Degrader-1 contains modified CRBN ligands, linker and Lenalidomide (HY-A0003)-linker fragments. PROTAC MLKL Degrader-1 abrogates cell death in a TSZ model of necroptosis.
    PROTAC MLKL Degrader-1
  • 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-161369
    CBPD-268 2832961-58-5 99.23%
    CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Structure Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker).
    CBPD-268
  • HY-168016
    PROTAC YAP degrader-1 3058483-58-9 99.77%
    PROTAC YAP degrader-1 (compound YZ-6) is a PROTAC targeting YAP and also inhibits the nuclear localization of YAP. PROTAC YAP degrader-1 is composed of PROTAC target protein ligand NSC682769 (HY-168017) (red part) and E3 ubiquitin ligase ligand + Linker conjugate (R,S,R)-AHPC-PEG2-C2-boc (HY-168019) (blue+black part), in which the PROTAC Linker used is Acid-PEG2-C2-Boc (HY-140480) and the target protein ligand activity control is Demethyl-NSC682769 (HY-168018)[1].
    PROTAC YAP degrader-1
  • HY-155815
    MS9715 99.48%
    MS9715 is a potent and seletive NSD3-targeting PROTAC. MS9715 is designed by BI-9321, which binds NSD3’s PWWP1 domain, with an E3 ligase VHL ligand. MS9715 has the potental for NSD3-dependent cancer treatment research.
    MS9715
  • HY-128841
    PROTAC MDM2 Degrader-2 2249944-99-6
    PROTAC MDM2 Degrader-2 is an MDM2 PROTAC degrader. PROTAC MDM2 Degrader-2 can induce the self-ubiquitination and degradation of MDM2, thereby upregulating the level of p53 protein. PROTAC MDM2 Degrader-2 has anti-tumor activity and can be used in the study of cancer. (Blue: MDM2 ligand (HY-128836); Black: linker (HY-128833))
    PROTAC MDM2 Degrader-2
  • HY-129966
    PROTAC IRAK4 degrader-1 2360533-90-8 99.77%
    PROTAC IRAK4 degrader-1 (compound I-210) is a Cereblon-based IRAK4 PROTAC. PROTAC IRAK4 degrader-1 is composed of IRAK4 ligand (red part) PROTAC IRAK4 ligand-1 (HY-129967), E3 ligase ligand (blue part) Pomalidomide (HY-10984), and PROTAC linker (black part) AM-Imidazole-PA-Boc (HY-129968).
    PROTAC IRAK4 degrader-1
  • HY-128756
    SIAIS178 2376047-73-1 99.36%
    SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.
    SIAIS178
  • HY-133137
    SJF620 2376187-16-3 98.98%
    SJF620 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
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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