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-181729
    PROTAC BET Degrader-15
    PROTAC BET Degrader-15 is a BET PROTAC degrader with DC50 values of <0.10 nM, <0.01 nM, and <0.01 nM against BRD2, BRD3, and BRD4, respectively. PROTAC BET Degrader-15 induces significant G2/M phase cell cycle arrest and triggers apoptosis. PROTAC BET Degrader-15 causes marked downregulation of c-Myc, accompanied by upregulation of the cell cycle inhibitory protein p21, downregulation of CDK6, and an increase in the apoptosis marker cleaved PARP. PROTAC BET Degrader-15 is applicable to the research of hematologic malignancies and lung cancer.
    PROTAC BET Degrader-15
  • HY-169086
    KL-465 3057446-82-6
    KL-465 is a MAGE-A3 PROTAC degrader that degrades MAGE-A3 in HeLa cells with a DC50 of 2 μM. KL-465 inhibits the proliferation of MAGE-A3-positive cancer cells. KL-465 can be used for the research of MAGE-A3-related cancers.
    KL-465
  • HY-181324
    PROTAC EZH2 Degrader-23 2653338-67-9
    PROTAC EZH2 Degrader-23 (compound 8) is a PROTAC protein degrader targeting EZH2 with a target IC50 of 30.00 nM. PROTAC EZH2 Degrader-23 inhibits EZH2 methyltransferase activity via interaction with the EZH2 SET domain.
    PROTAC EZH2 Degrader-23
  • HY-179321
    PROTAC HDAC4 Degrader-1 3036245-14-1
    PROTAC HDAC4 Degrader-1 (compound SCT-1) is a potent and selective PROTAC HDAC4 degrader. PROTAC HDAC4 Degrader-1 reduces HDAC4 protein level, induces S phase cell cycle arrest, and inhibits cell colony formation, thereby inhibiting proliferation of the tumor cells. PROTAC HDAC4 Degrader-1 exhibits efficacy in a H460 mouse model. PROTAC HDAC4 Degrader-1 can be used for cancer research, such as lung cancer.
    PROTAC HDAC4 Degrader-1
  • HY-163868
    PROTAC SMARCA2/4-degrader-15 2568276-81-1
    PROTAC SMARCA2/4-degrader-15 (Compound I-335) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-15 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM
    PROTAC SMARCA2/4-degrader-15
  • HY-159461
    PROTAC SMARCA2/4-degrader-9 2568507-15-1
    PROTAC SMARCA2/4-degrader-9 (Compound I-503) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2 degrader-9 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM.
    PROTAC SMARCA2/4-degrader-9
  • HY-174210
    PROTAC BRD4 Degrader-31
    PROTAC BRD4 Degrader-31 is a BRD4 PROTAC degrader with DC50 s of 164 and 80 nM at 4 h and 24 h, respectively. PROTAC BRD4 Degrader-31 potently degrades BRD4 in cells with long acting degradation kinetics. Pink: BRD4 ligand (HY-78695); Blue: KLHDC2 ligand (HY-174218)
    PROTAC BRD4 Degrader-31
  • HY-169274
    PROTAC SMARCA2 degrader-23 2892523-67-8
    PROTAC SMARCA2 degrader-23 (Example 1) is a potent and selective PROTAC SMARCA2 degrader，with a DC50 of <100 nM. PROTAC SMARCA2 degrader-23 has the potential for the research of cancer.
    PROTAC SMARCA2 degrader-23
  • HY-138637
    PROTAC BRD4 Degrader-14 3026420-43-6
    PROTAC BRD4 Degrader-14 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.8 nM and 1.7 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-14 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
    PROTAC BRD4 Degrader-14
  • HY-170340
    PROTAC ER Degrader-14 2504911-73-1
    PROTAC ER Degrader-14 (compound 86) is a PTORAC-type Estrogen Receptor/ERR degrader.
    PROTAC ER Degrader-14
  • HY-174315
    WZH-17-002
    WZH-17-002 is a WZH-15-125-based ALK PROTAC degrader with a DC50 of 25 nM. WZH-17-002 enhances activities against Lorlatinib (HY-12215)-resistant ALK compound mutations. WZH-17-002 significantly reduces drug resistance in ALK-fusion non-small cell lung cancer (NSCLC) and inhibits tumor growth in EML4-ALK G1202R/L1196 M xenograft mice model. Pink: ALK ligand (HY-174314); Blue: CRBN ligase ligand (HY-14658); Black: linker (HY-174316)
    WZH-17-002
  • HY-159015
    SIAIS630120-NC
    SIAIS630120-NC is a negative control for NAMPT (nicotinamide phosphoribosyltransferase) degrader SIAIS630120.
    SIAIS630120-NC
  • HY-153321A
    (R,R)-Bexobrutideg 2649400-33-7 98.83%
    (R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker).
    (R,R)-Bexobrutideg
  • HY-175455
    LYA914
    LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458).
    LYA914
  • HY-170995
    PROTAC ROR1 degrader-1
    PROTAC ROR1 degrader-1 is a ROR1 PROTAC degrader with DC50 values of 40.88 nM (NCI-H23), 69.0 nM (NCI-H460), 83.35 nM (NCI-H1299) and 42.07 nM (NCI-H1975), respectively. PROTAC ROR1 degrader-1 inhibits the proliferation of lung cancer cells and induces apoptosis. PROTAC ROR1 degrader-1 can be used in research related to non-small cell lung cancer.
    PROTAC ROR1 degrader-1
  • HY-181967
    PROTAC PARP1 degrader-5
    PROTAC PARP1 degrader-5 is a PARP1 PROTAC degrader with a DC50 of 0.12 μM. PROTAC PARP1 degrader-5 hijacks the ubiquitin-proteasome system via catalytic ternary complex formation to drive sustained PARP1 degradation. PROTAC PARP1 degrader-5 induces DNA damage, drives marginal cytosolic double-stranded DNA accumulation in tumor cells, and up-regulates PD-L1 surface expression in tumor cells. PROTAC PARP1 degrader-5 shows tumor growth inhibition activity in murine melanoma models when encapsulated in lipid nanoparticles. PROTAC PARP1 degrader-5 can be used for the research of cancer, such as melanoma.
    PROTAC PARP1 degrader-5
  • HY-179233
    PROTAC STAT6 degrader-2 3105288-31-8
    PROTAC STAT6 degrader-2 is a highly efficient PROTAC degrader targeting STAT6. PROTAC STAT6 degrader-2 has a DC50 value of 1-10 nM for STAT6 in human PBMC cells and a DC50 value of less than 100 nM for STAT6 in HEK293-HIBiT-STAT6 cells. PROTAC STAT6 degrader-2 can be used for STAT6-mediated diseases.
    PROTAC STAT6 degrader-2
  • HY-181767
    PROTAC HDAC3 degrader-1
    PROTAC HDAC3 degrader-1 is a selective PROTAC degrader targeting HDAC3 with a DC50 of 30.73 nM. PROTAC HDAC3 degrader-1 induces degradation of HDAC3 via the ubiquitin-proteasome system. PROTAC HDAC3 degrader-1 promotes apoptosis, induces DNA damage, and downregulates anti-apoptotic proteins Mcl-1 and Bcl-xL. PROTAC HDAC3 degrader-1 can be used for the research of acute myeloid leukemia.
    PROTAC HDAC3 degrader-1
  • HY-171824
    PROTAC c-Met Degrader-4 2959535-15-8
    PROTAC c-Met Degrader-4 (compound D15) is a potent orally active PROTAC c-MET degrader. PROTAC c-Met Degrader-4 demonstrates excellent intracellular degradation potency with a DC50 < 0.5 nM. PROTAC c-Met Degrader-4 induces cell cycle arrest and apoptosis, inhibits cell invasion and migration, thereby suppressing cell proliferation. PROTAC c-Met Degrader-4 inhibits the growth of Hs746T xenograft tumors in nude mice. PROTAC c-Met Degrader-4 can be used for cancer research, such as non-small cell lung cancer and gastric cancer.
    PROTAC c-Met Degrader-4
  • HY-153425
    PROTAC SMARCA2/4 degrader-41 2892523-74-7
    PROTAC SMARCA2/4 degrader-41 is a SMARCA2/4 PROTAC degrader with a DC50 and IC50 both < 0.1 μM. PROTAC SMARCA2/4 degrader-41 is applicable to research on SMARCA2/4-related or SMARCA2/4-deficient cancers.
    PROTAC SMARCA2/4 degrader-41
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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