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-168540
    PROTAC MPS1 degrader 1
    PROTAC MPS1 degrader 1 (Compound 19) is a potent degrader of monopolar spindle 1 (Mps1, TTK), AURKA and AURKB, with DC50s of 17.7, 108.7 and 570.3 nM, respectively. PROTAC MPS1 degrader 1 can be used for the research of acute myeloid leukemia. (Pink: ligand for target protein (HY-168542); Black: linker (HY-W141926); Blue: ligand for E3 ligase (HY-10984).
    PROTAC MPS1 degrader 1
  • HY-168556
    YJ9069
    YJ9069 is a selective CDK12/CDK13 PROTAC degrader with an IC50 of 22.22 nM for in VCaP cells. CDK12/13 degradation rapidly triggers gene-length-dependent transcriptional elongation defects, leading to DNA damage and cell-cycle arrest. YJ9069 effectively inhibits proliferation in subsets of prostate cancer cells and significantly suppresses prostate tumor growth. (Pink: CDK12/CDK13 degradation agent (HY-168658); Black: Linker (HY-W015967); Blue: ligand for E3 ligase (HY-103596)).
    YJ9069
  • HY-173266
    TO-1187
    TO-1187 is a selective HDAC6 PROTAC degrader (DC50: 5.81 nM). TO-1187 promotes the ubiquitination and degradation of HDAC6 and can be used in the study of hematological malignancies and solid tumors (Pink: HDAC6 ligand (HY-173386); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-140212)).
    TO-1187
  • HY-168969
    AA-BR-157
    AA-BR-157 is a PROTAC degrader for metallothionein 2A (MT2A) with a DC50 of 190 nM. AA-BR-157 downregulates the cytoskeleton and cell motility regulating protein DIAPH3, inhibits the migration of MDA-MB-231 and U-87 MG. AA-BR-157 regulates the zinc homeostasis in MDA-MB-231. (Pink: ligand for target protein MT2A ligand 1 (HY-168970); Black: linker (HY-119429); Blue: ligand for VHL E3 ligase (HY-125845))
    AA-BR-157
  • HY-141797
    MS33 2407449-11-8
    MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia.
    MS33
  • HY-145819
    JPS036 2669785-85-5
    JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
    JPS036
  • HY-162749
    G9D-4
    G9D-4 is a potent PROTAC degrader of G9a, with the DC50 value of 0.1 μM in PANC-1 cells and do not directly perturb GLP protein, with the DC50 of ＞10 μM. G9D-4 plays an important role in pancreatic cancer research (Pink: Ligand for target protein G9a/GLP Inhibitor (HY-15273); Black: Linker; Blue: Ligand for E3 ligase (HY-10984)).
    G9D-4
  • HY-168546
    CFT-1297 2154353-03-2
    CFT-1297 is a BET PROTAC degrader that can degrade BRD4.
    CFT-1297
  • HY-174864
    JP-163-16
    JP-163-16 is a RelA/p65 PROTAC degrader. JP-163-16 selectively reduces the expression of RelA/p65 in a proteasome-dependent manner in cells. JP-163-16 can induce cell apoptosis by inhibiting the NF-κB signaling pathway. JP-163-16 can be used for research on RelA/p65-dependent tumours, such as chronic lymphocytic leukaemia (CLL). (Pink: RelA/p65 Ligand (HY-174865); Blue: CRBN Ligand (HY-A0003); Black: Linker; CRBN Ligand+Linker (HY-160241)).
    JP-163-16
  • HY-139620A
    MS83 epimer 1 98.36%
    MS83 epimer 1 is the epimer of MS83 (HY-139620). MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.
    MS83 epimer 1
  • HY-158381
    PROTAC PTP1B degrader 1 99.37%
    PROTAC PTP1B degrader 1 (compound 75) is a CRBN-based PTP1B PROTAC degrader, with DC50 values of 0.2 μM (48 h) and 0.05 μM (72 h) (Red: PTP1B ligand Oleanolic acid (HY-N0156); Black: linker; Blue: CRBN ligand).
    PROTAC PTP1B degrader 1
  • 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-173333
    PROTAC SMARCA2/4 degrader-38 3081688-77-6
    PROTAC SMARCA2/4 degrader-38 is a degrader SMARCA2/4 PROTAC (DC50: 3.0 nM and 4.0 nM respectively). PROTAC SMARCA2/4 degrader-38 promotes the ubiquitination and degradation of SMARCA2/4. PROTAC SMARCA2/4 degrader-38 blocks the G0/G1 cell cycle and induces apoptosis. PROTAC SMARCA2/4 degrader-38 can be used in acute myeloid leukemia (AML) research. (Pink: SMARCA2/4 ligand; Blue: VHL ligand (HY-112078); Black: linker; Target Protein Ligand-Linker Conjugates (HY-173343)).
    PROTAC SMARCA2/4 degrader-38
  • HY-171830
    MS105 2408339-39-7
    MS105 (YX39-105) is an orally active and selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. MS105 recruits VHL E3 ligase via the VHL ligand moiety to promote PTK6 ubiquitination and proteasomal degradation, inhibiting breast cancer cell proliferation, migration, and inducing apoptosis. MS105 is promising for research of breast cancer. (Pink: BRK inhibitor P21d hydrochloride (HY-115514); Black: linker (HY-W105727); Blue: (S,R,S)-AHPC (HY-125845)).
    MS105
  • HY-164864
    DU-14 (PTP1B/TC-PTP PROTAC) 3053413-58-1
    DU-14 (PTP1B/TC-PTP PROTAC) is a potent and selective PTP1B and TC-PTP dual PROTAC degrader. DU-14 (PTP1B/TC-PTP PROTAC) has the IC50 for PTP1B and TC-PTP phosphatase activity of 24.2 nM and 30.1 nM, respectively. DU-14 (PTP1B/TC-PTP PROTAC) enhances IFN-γ signaling, promotes T cell activation, and has anti-tumor activity. (Pink: PTP1B/TC-PTP inhibitor (HY-171027); Black: Linker (HY-W340290); Blue: E3 ligand (HY-112078)).
    DU-14 (PTP1B/TC-PTP PROTAC)
  • HY-153932
    NR-7h 2550399-06-7
    NR-7h is a potent and selective p38α and p38β degrader with DC50 values of 24 nM and 27.2 nM for p38α in T47D, MB-MDA-231 cells, respectively.
    NR-7h
  • HY-114405
    SJFδ 2254609-23-7
    SJFδ is a 10-atom linker PROTAC based on von Hippel-Lindau ligand. SJFδ degrades p38δ with a DC50 of 46.17 nM, but does not degrade p38α, p38β, or p38γ.
    SJFδ
  • HY-155113
    PROTAC Hsp90α degrader 1 3031078-90-4 98.30%
    PROTAC Hsp90α degrader 1 (Compound X10g) is a selective PROTAC Hsp90α degrader. PROTAC Hsp90α degrader 1 can be used for breast cancer research. PROTAC Hsp90α degrader 1 inhibits the proliferation of MDA-MB-231, MDA-MB-468, MCF-7, MX-1 cells with IC50s of 51.48 μM, 16.46 μM, 8.93 μM, 11.95 μM respectively.
    PROTAC Hsp90α degrader 1
  • HY-163985
    PROTAC FGFR2 degrader 1 3099123-99-3
    PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM. PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) .
    PROTAC FGFR2 degrader 1
  • HY-149760
    PVD-06 3032975-48-4 98.30%
    PVD-06 is a selective PROTAC PTPN2 degrader with a DC50 of 217 nM (selectivity index >60-fold over PTP1B). PVD-06 induces PTPN2 degradation via a VHL-, ubiquitin, and proteasome-dependent pathway. PVD-06 can promote T cell activation and amplify IFN-γ-mediated anticancer activity. PVD-06 can be used to further investigate PTPN2 in diseases such as leukemia and melanoma. (Pink: PTPN2 ligand (HY-168691), Black: linker (HY-B0236), Blue: VHL ligand (HY-112078)).
    PVD-06
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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