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-180969
    SIAIS056 2378581-37-2
    SIAIS056 is a BCR-ABL PROTAC degrader with a DC50 value of 0.18 nM. SIAIS056 time-dependently inhibits the BCR-ABL signaling pathway, accompanied by decreased phosphorylation of BCR-ABL and the downstream molecules STAT5 and CRKL in K562 cells. SIAIS056 induces the degradation of several clinically relevant resistance-conferring mutations of BCR-ABL. SIAIS056 exhibits anti-proliferative activity and induces substantial tumor regression in K562 xenograft models. SIAIS056 can be used for leukemia research.
    SIAIS056
  • HY-168246
    PROTAC SMARCA2 degrader-29 2865193-25-3
    PROTAC SMARCA2 degrader-29 (Example 87) is a PROTAC SMARCA2 (BRM) degrader, with DC50 of 10-100 nM (BRM) and > 1 μM (BRG1, also known as SMARCA2) respectively.
    PROTAC SMARCA2 degrader-29
  • HY-180850
    ERB-2
    ERB-2 is a selective ERβ PROTAC degrader. ERB-2 removes the inhibitory effect of ERβ on ROS, leading to the accumulation of ROS, mitochondrial damage, and ultimately triggering cell apoptosis (apoptosis). ERB-2 significantly inhibits tumor growth in the nude mouse model of NCI-H1975OR tumors. ERB-2 can be used for the study of non-small cell lung cancer.
    ERB-2
  • HY-185358
    PROTAC MALT1 Degrader-1 2975664-37-8
    PROTAC MALT1 Degrader-1 (Compound 176) is a MALT1 PROTAC degrader. PROTAC MALT1 Degrader-1 is applicable to lymphoma research.
    PROTAC MALT1 Degrader-1
  • HY-168255
    PROTAC BRM/BRG1 degrader-4
    PROTAC BRM/BRG1 degrader-4 (example 047) is a potent BRM and BRG1 PROTAC degrader, with DC50 values of 0.21 nM and 3.4 nM in SW1573 cells, respectively.
    PROTAC BRM/BRG1 degrader-4
  • HY-168551
    PROTAC ALK degrader-3
    PROTAC ALK degrader-3 (4B) is an orally active ALK degrader based on PROTACs, which can effectively induce persistent degradation of ALK fusion protein in Karpas 299 cells and strong inhibition of downstream pathways,IC50 is 119.33 nM. PROTAC ALK degrader-3 exhibits antitumor activity. (Structure Note: PINK, ALK Inhibitor (HY-15656); Blue, E3 (HY-W023573); Black, linker (HY-168552)).
    PROTAC ALK degrader-3
  • HY-175281
    SJ11646 2933135-82-9
    SJ11646 is a Dasatinib (HY-10181)-based LCK PROTAC degrader with a DC50 of 0.00838 pM. SJ11646 has potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples with drastically prolonged suppression of LCK signaling, and induces T-ALL apoptosis. SJ11646 binds to 51 human kinases with a high affinity (particularly ABL1, KIT, and DDR1). SJ11646 has superior antileukemic efficacy in T-ALL mice model. . Pink: LCK ligand (HY-107447); Blue: CRBN ligase ligand (HY-163169); Black: linker (HY-76667)
    SJ11646
  • HY-168229
    PROTAC SMARCA2 degrader-27 2410314-57-5
    PROTAC SMARCA2 degrader-27 (compound 4) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-27 has the potential to be used in cancer research.
    PROTAC SMARCA2 degrader-27
  • HY-148777
    A031 2682255-44-1
    A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP).
    A031
  • HY-169133
    GDCNF-11 2991588-80-6
    GDCNF-11 is a HIM-PROTAC GPX4 degrader based on the chaperone protein HSP90. GDCNF-11 promotes the ubiquitination and degradation of GPX4 through the HSP 90 chaperone complex, reduces endogenous GPX4 expression to induce ferroptosis in HT-1080 cells, and the DC50 value is 0.08 μM (Pink: Target protein ligand (HY-153748); Blue: HSP90 ligand (HY-10212); Black: Linker (HY-W169526)).
    GDCNF-11
  • HY-161498
    XYD198
    XYD198 (Compound 14h) is an orally active degrader for CBP/p300. XYD198 inhibits CBP/p300 bromodomain with IC50 of 213.5 nM. XYD198 exhibits antitumor activity against acute myeloid leukemia.
    XYD198
  • HY-159651
    PTOTAC HSD17B13 degrader 1 3046195-01-8
    PTOTAC HSD17B13 degrader 1 (compound 1) is a PROTAC targeting 17β-HSD 13 (HSD17B13). PTOTAC HSD17B13 degrader 1 is composed of PROTAC target protein ligand HSD17B13 degrader 2 (HY-159662) (red part), PROTAC Linker tert-Butyl 5-bromoisoindoline-2-carboxylate (HY-W003696) (black part) and E3 ubiquitin ligase ligand E3 ligase Ligand 31 (HY-159660) (blue part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 114 (HY-159661)[1].
    PTOTAC HSD17B13 degrader 1
  • HY-178459
    PROTAC HPK1 Degrader-6 3099168-12-1
    PROTAC HPK1 Degrader-6 (314) is a highly efficient and effective PROTAC degrader targeting HPK1 (IC50 ＜ 50 nM). PROTAC HPK1 Degrader-6 can be used for the study of leukemia. Red: HPK1 ligand (HY-179196); Blue: E3 ligase CRBN ligand (HY-179197).
    PROTAC HPK1 Degrader-6
  • HY-182275
    PROTAC PRMT1 degrader-1
    PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma.
    PROTAC PRMT1 degrader-1
  • HY-183783
    PROTAC RET Degrader 2
    PROTAC RET Degrader 2 is a RET degrader with a target IC50 of 0.36 nM. PROTAC RET Degrader 2 is mainly composed of RET-IN-34 (HY-183729) and Thalidomide (HY-14658). PROTAC RET Degrader 2 mediates RET degradation via the ubiquitin-proteasome system. PROTAC RET Degrader 2 induces apoptosis, inhibits colony-forming ability, and exhibits antiproliferative activity in cancer cells. PROTAC RET Degrader 2 suppresses tumor growth in xenograft models. PROTAC RET Degrader 2 can be used in research related to medullary thyroid carcinoma, papillary thyroid carcinoma, and RET fusion-positive lung adenocarcinoma.
    PROTAC RET Degrader 2
  • HY-182331
    WCF-598 3059574-58-9
    WCF-598 is a RXRγ (Kd: 234.2 nM) PROTAC degrader. WCF-598 induces RXRγ degradation via the ubiquitin-proteasome pathway and binds directly to RXRγ. WCF-598 indirectly induces AR-V7 degradation, impairs the stability of the RXRγ-AR-V7 complex, downregulates AR-V7 levels, and inhibits the transcription of downstream target genes of AR-V7. WCF-598 induces tumor cell apoptosis, inhibits cell proliferation, activates the p53 signaling pathway, and suppresses cell cycle progression. WCF-598 can be used for the research of prostate cancer.
    WCF-598
  • HY-184342
    SYC-2863
    SYC-2863 is a CRBN-recruiting PROTAC degrader that selectively degrades ENL (MLLT1), with an ENL DC50 of 45 nM in MV4;11 cells. SYC-2863 inhibits the proliferation of MLL-rearranged leukemia and multiple myeloma cells. After degrading intracellular ENL, SYC-2863 dose-dependently downregulates the transcription levels of MYC and its downstream target genes, blocking the MYC-mediated malignant proliferation pathway. SYC-2863 can be used in studies related to MLL-rearranged leukemia and multiple myeloma.
    SYC-2863
  • HY-180960
    NEP202 3031840-41-9
    NEP202 is a SMARCA2 PROTAC degrader designed based on the GID4 E3 ligase. NEP168 can be used for cancer research.
    NEP202
  • HY-149870
    PROTAC CDK9 degrader-8 2994191-89-6
    PROTAC CDK9 degrader-8 (compound 21) is a potent PROTAC CDK9 degrader with an IC50 value of 0.01 μM. PROTAC CDK9 degrader-8 can be used in research of cancer.
    PROTAC CDK9 degrader-8
  • HY-185634
    PROTAC GSK3 degrader-1
    PROTAC GSK3 degrader-1 is a potent, blood-brain barrier-permeable GSK3 PROTAC degrader, with a DC50 of 1.4 nM against GSK3β. PROTAC GSK3 degrader-1 exerts equally potent degradation activity against both GSK3α and GSK3β. It inhibits the phosphorylation of CRMP2, PRKAA1 and Tau, and stabilizes β-catenin. PROTAC GSK3 degrader-1 can be used in the research of Alzheimer's disease and Parkinson's disease.
    PROTAC GSK3 degrader-1
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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