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-114312
    MD-224 2136247-12-4 99.60%
    MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent. MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MD-224
  • HY-141680
    CPS2 2756741-90-7 99.33%
    CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC50= 24 nM). CPS2 can be used for the research of acute myeloid leukemia.
    CPS2
  • HY-153220
    NX-2127 2416131-46-7 99.72%
    NX-2127 (compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . NX-2127 inhibits proliferation of BTKC481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells. NX-2127 is composed of PROTAC target protein ligand (red part) BTK ligand 10 (HY-168302), E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383) and PROTAC Linker (black part) (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303). Among which, the conjugate of E3 ubiquitin ligase ligand + Linker compose of Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304).
    NX-2127
  • HY-133129
    MS1943 2225938-17-8 98.92%
    MS1943 is an orally active, PROTAC-based, selective degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC50=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458); Blue, Hyt (HY-W001578)).
    MS1943
  • HY-123937
    THAL-SNS-032 2139287-33-3 99.16%
    THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
    THAL-SNS-032
  • HY-153367
    FHD-609 2676211-64-4 99.15%
    FHD-609 is a PROTAC degrader and inhibitor of BRD9 (Bromodomain-containing protein 9). FHD-609 targets to ncBAF, can be used for research of wide range of cancers that contain a mutation in a BAF complex subunit. FHD-609 in combination with Telomelysin or INO5401, may play a role in adrenocortical carcinoma (ACC) treatment. (Blue: BRD9 ligand-6 (HY-49393), Black: linker (HY-168309); Pink: (S)-Deoxy-thalidomide-Br (HY-168308) ).
    FHD-609
  • HY-137516
    LC-2 2502156-03-6 98.16%
    LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines.
    LC-2
  • HY-139039
    BSJ-4-116 2519823-34-6 98.73%
    BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162).
    BSJ-4-116
  • HY-139156
    SK-575 2523016-96-6 99.86%
    SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations.
    SK-575
  • HY-141796
    MS67 2407452-77-9 98.73%
    MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.
    MS67
  • HY-122826
    ZXH-3-26 2243076-67-5 98.90%
    ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM.
    ZXH-3-26
  • HY-158101
    BMS-986365 2446928-30-7 99.92%
    BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader, capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. (Blue: HY-W247437; Black: linker (HY-W126831); Pink: HY-168697).
    BMS-986365
  • HY-153321
    NX-5948 2649400-34-8 99.33%
    NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker).
    NX-5948
  • HY-141881
    PROTAC-O4I2 2785323-62-6 99.66%
    PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells.
    PROTAC-O4I2
  • HY-151623
    ACBI2 2913161-19-8 99.76%
    ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. ACBI2 can be used in the research of lung cancer.
    ACBI2
  • HY-P5819A
    xStAx-VHLL TFA 99.22%
    xStAx-VHLL TFA is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL TFA inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL TFA can inhibit the proliferation of colon cancer cells and has anti-tumor activity.
    xStAx-VHLL TFA
  • HY-130708
    UNC6852 2688842-08-0 99.60%
    UNC6852 is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a von Hippel-Lindau ligand, with an IC50 of 247 nM for EED.
    UNC6852
  • HY-158105
    ARV-393 2851885-95-3 99.15%
    ARV-393 is a potent and orally active BCL6 PROTAC degrader. ARV-393 induces ubiquitination of BCL6 and its subsequent degradation by the proteasome. ARV-393 has the potential for the research of advanced non-hodgkin lymphoma.
    ARV-393
  • HY-132296
    GSK215 2743427-26-9 99.26%
    GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.
    GSK215
  • HY-148813
    AK-2292 2984506-77-4 99.73%
    AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models. AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    AK-2292
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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