PROTACs
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
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PROTACs 관련 제품 (1355)
관련 제품 (1355)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC DYRK2 degrader-2
0 ImagesPROTAC DYRK2 degrader-2 is a PROTAC DYRK2 degrader based on curcumin analog A3. It recruits the CRBN E3 ligase to mediate DYRK2 ubiquitination and achieves degradation via the ubiquitin-proteasome system. PROTAC DYRK2 degrader-2 downregulates the expression level of DYRK2 protein in cancer cells. It is applicable to cancer-related research.
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PROTAC BRD4 Degrader-31
0 ImagesCat. No.: HY-174210PROTAC BRD4 Degrader-3 is a potent BRD4 PROTAC degrader with DC50 values of 164 nM and 80 nM at 4 h and 24 h, respectively. PROTAC BRD4 Degrader-3 induces the ubiquitination and subsequent proteasomal degradation of BRD4 by recruiting the ubiquitin E3 ligase KLHDC2. PROTAC BRD4 Degrader-3 can be used in breast cancer research.
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PROTAC BRD4 Degrader-14
0 ImagesCat. No.: HY-138637CAS No.: 3026420-43-6
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PROTAC ER Degrader-14
0 ImagesCat. No.: HY-170340CAS No.: 2504911-73-1PROTAC ER Degrader-14 (compound 86) is a PTORAC-type Estrogen Receptor/ERR degrader.
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WZH-17-002
0 ImagesCat. No.: HY-174315WZH-17-002 is a CRBN‑recruiting ALK PROTAC degrader. WZH‑17‑002 degrades ALK proteins, including EML4‑ALK and the compound mutants. WZH‑17‑002 inhibits the development of drug resistance in ALK‑fusion non‑small‑cell lung cancer. WZH‑17‑002 can be used for research related to non‑small‑cell lung cancer.
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(R,R)-Bexobrutideg
0 ImagesSynonyms: (R,R)-NX-5948; (R,R)-BTK-IN-24(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).
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LYA914
0 ImagesCat. No.: HY-175455LYA914 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).
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PROTAC ROR1 degrader-1
0 ImagesCat. No.: HY-170995PROTAC 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.
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PROTAC PARP1 degrader-5
0 ImagesCat. No.: HY-181967PROTAC 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.
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PROTAC HDAC3 degrader-1
0 ImagesCat. No.: HY-181767PROTAC 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.
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PROTAC c-Met Degrader-4
0 ImagesCat. No.: HY-171824CAS No.: 2959535-15-8PROTAC 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.
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MA203
0 ImagesCat. No.: HY-179157MA203 is a highly efficient and selective PROTAC degrader targeting CHK1. MA203 accelerates CRBN-dependent proteasomal degradation of CHK1 in solid tumor-derived cells and acute leukemia cells. MA203 induces DNA replication stress. MA203 blocks cell cycle progression and triggers tumor cell apoptosis. MA203 does not damage healthy differentiated and primitive hematopoietic cells, stromal cells, and retinal epithelial cells. MA203 can be used for the study of CHK1-dependent cancers.
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GXF-111
0 ImagesCat. No.: HY-153414GXF-111 is a BRD3 and BRD4-L PROTAC degrader. Its BD1 and BD2 Ki values against human BRD3 are 11.97 nM and 2.45 nM, respectively. The degradation activity of GXF-111 depends on its binding to BET proteins and Cereblon, as well as the involvement of a functional proteasome. The degradation selectivity of GXF-111 is mainly determined by differences in degradation kinetics and cell types. GXF-111 induces G1 phase cell cycle arrest, downregulates c-Myc expression, upregulates p21 expression, and exhibits antiproliferative activity against a variety of cancer cell lines. GXF-111 can serve as a research tool for cancer-related studies.
