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-135309
    PROTAC ER Degrader-4 2361114-15-8 98.78%
    PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM.
    PROTAC ER Degrader-4
  • HY-137346
    DD-03-156 2769753-69-5 99.90%
    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-161536
    PROTAC EGFR degrader 9 2992670-33-2 98.35%
    PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFRL858R/T790M/C797S. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537)).
    PROTAC EGFR degrader 9
  • HY-151110
    PROTAC CDK12/13 Degrader-1 98.01%
    PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research.
    PROTAC CDK12/13 Degrader-1
  • HY-148065
    FMF-06-098-1 2769753-07-1 98.77%
    FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1 (Pink: target protein ligand (HY-169396); Blue: VHL ligand (HY-112078); Black: Linker (HY-124380)).
    FMF-06-098-1
  • HY-159779
    NR-V04 2766608-52-8
    NR-V04 is a PROTAC based NR4A1 degrader (Red: NR4A1 inhibitor (HY-13067), black: linker, Blue: E3 ligase ligand).
    NR-V04
  • HY-162704
    JMV7048 2871774-88-6 99.12%
    JMV7048 is an effective PROTAC degrader targeting PXR (Pregnane X Receptor) with a DC50 of 379 nM. JMV7048 induces the polyubiquitination and degradation of PXR protein by recruiting E3 CRBN ubiquitin ligase and the 26S proteasome. JMV7048 significantly enhances the sensitivity of colon cancer stem cells to chemotherapy by reducing the expression of PXR protein in these cells, thereby significantly delaying cancer recurrence in vivo. JMV7048 is composed of the PXR agonist JMV6944 (HY-162738), linker (HY-162736), and Thalidomide 5-fluoride (HY-W087383) (Red: JMV6944; Blue: Thalidomide 5-fluoride ligand; Black: linker).
    JMV7048
  • HY-158142
    PROTAC TYK2 degrader-1 2770470-20-5 99.55%
    PROTAC TYK2 degrader-1 (CPD-155) is a PROTAC targeting degrader to TYK2 with Dmax >60%. (Structure Note: PINK, TYK2 ligand 1 (HY-158340); Blue, VHL ligand Thalidomide (HY-14658); Black, linker)
    PROTAC TYK2 degrader-1
  • HY-147099
    dTAG-47-NEG
    dTAG-47-NEG is an analog of dTAG-47 that cannot bind and recruit cereblon (CRBN). dTAG-47-NEG can be used as a heterobifunctional negative control of dTAG-47.
    dTAG-47-NEG
  • HY-155218
    TMX-2172 2488892-09-5 99.38%
    TMX-2172 is a PROTACs degrader for CDK2 and CDK5, with the IC50s of 6.5 and 6.8 nM, respectively. TMX-2172 plays an important role in cancer research (Blue: E3 ligase ligand (HY-W008352); Pink: target protein ligand (HY-170748); Black: linker (HY-151072)).
    TMX-2172
  • HY-152134
    HDAC6 degrader-3 2785404-83-1 98.60%
    HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. HDAC6 degrader-3 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin.
    HDAC6 degrader-3
  • HY-144691
    PP-C8 3032108-74-7 99.99%
    PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC).
    PP-C8
  • HY-171140
    PROTAC HDAC6 degrader 3 99.81%
    PROTAC HDAC6 degrader 3 (Compound 4) is a selective inhibitor and degrader for HDAC6 with an IC50 of 686 nM and a DC50 of 171 nM. PROTAC HDAC6 degrader 3 promotes the acetylation of α-tubulin. (Pink: ligand for target protein (HY-171141); Blue: ligand for E3 ligase VHL (HY-150803))
    PROTAC HDAC6 degrader 3
  • HY-168162
    ZLC491 3053716-46-1 98.51%
    ZLC491 is an orally active CDK12/13 PROTAC degrader. ZLC491 can be used in anticancer research.
    ZLC491
  • HY-156152A
    CARM1 degrader-1 hydrochloride 99.44%
    CARM1 degrader-1 hydrochloride is the hydrochloride salt form of CARM1 degrader-1 (HY-156152). CARM1 degrader-1 hydrochloride is a PROTAC degrader for co-activator associated argininemethyltransferase 1 (CARM1), which degrades CARM1 in a VHL- and proteasome-dependent manner with a DC50 of 8.1 nM. CARM1 degrader-1 hydrochloride inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, and thus inhibits breast cancer cell migration.
    CARM1 degrader-1 hydrochloride
  • HY-145737A
    PROTAC SOS1 degrader-1 TFA 99.38%
    PROTAC SOS1 degrader-1 (TFA) is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity.
    PROTAC SOS1 degrader-1 TFA
  • HY-168660
    CPD-10 3055471-57-0
    CPD-10 is a potent CCND1 and CDK4 PROTAC degrader. CPD-10 shows anti-proliferation. CPD-10 induces apoptosis. CPD-10 decreases the protein expression of cyclin D1, cyclin D3, CDK4, P-Rb(5807/811) in a dose-dependent manner. (Pink: ligand for target protein (HY-50767); black: linker (HY-22391); Blue: E3 ligase ligand (HY-168667)).
    CPD-10
  • HY-115718
    PZ703b 2471970-56-4 98.00%
    PZ703b is a Bcl-xl PROTAC degrader that induces apoptosis and inhibits cancer cell proliferation. PZ703b can be used for the research of bladder cancer research.
    PZ703b
  • HY-158045
    PROTAC PARP1 degrader-1 99.86%
    PROTAC PARP1 degrader-1 (Compound CN0) is a PROTAC degrader of PARP1. PROTAC PARP1 degrader-1 activates the cGAS/STING immunity pathway and eventually enhances T cell killing of tumor cells. PROTAC PARP1 degrader-1 inhibits DNA damage repair, resulting in highly efficient accumulation of cytosolic DNA fragments (Blue: CRBN ligand, Black: linker; Pink: PARP1 inhibitor).
    PROTAC PARP1 degrader-1
  • HY-148063
    DB0614 2769753-47-9 98.80%
    DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade 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. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity.(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))
    DB0614
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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