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 Related Products (1398)
Related Products (1398)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC EGFR degrader 13
0 ImagesCat. No.: HY-158313CAS No.: 2861227-35-0PROTAC EGFR degrader 13 (compound 106) is an EGFR PROTAC degrader with a DC50 of <0.1 μM. PROTAC EGFR degrader 13 has proliferation inhibitory activity on cell Ba/F3-TEL-EGFR-T790M-L858R-C797S with an IC50 of 15.6 nM. PROTAC EGFR degrader 13 can be used for the study of EGFR-related diseases such as cancer.
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BTR2038
0 ImagesCat. No.: HY-178043BTR2038 is a BTR2000-based heterobifunctional PROTAC that induces the degradation of BRD9 by recruiting the CUL3KLHL20 E3 ubiquitin ligase. BTR2038 consists of a BRD9 bromodomain ligand derived from a BI-7273 analog, a linker, and the macrocyclic KLHL20 ligand BTR2000. BTR2038 is applicable for research related to KLHL20-recruited targeted protein degradation and BRD9 modulation.
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HRG038
0 ImagesCat. No.: HY-176070HRG038 is a covalent CUL4DCAF16-base PROTAC-liked BRD4 degrader. HRG038 induces proteasome- and Cullin E3 ligase-dependent degradation, covalently targets cysteine residue C173 on DCAF16 to mediate BRD4 degradation, and induces reduction in BRD3 levels. HRG038 shows selective loss of the short BRD4 isoform over the long isoform in non-cancer cells, degrades both BRD4 isoforms in breast cancer cells, and does not impair cell viability in non-cancer cells. HRG038 can be used for the research of breast cancer.
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PROTAC NSD2 degrader-1
0 ImagesCat. No.: HY-184968CAS No.: 3108071-48-0PROTAC NSD2 degrader-1 is a PROTAC degrader that selectively targets NSD2, with a DC50 of 0.37 μM. PROTAC NSD2 degrader-1 induces selective degradation of long and short isoforms of NSD2 containing the PWWP1 domain by forming a ternary complex with FBXO22. NSD2 degradation mediated by PROTAC NSD2 degrader-1 depends on the ubiquitin-proteasome system and the neddylation pathway. PROTAC NSD2 degrader-1 can be used in cancer-related research such as non-small cell lung cancer, multiple myeloma and prostate cancer.
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ZSH-2117
0 ImagesCat. No.: HY-174415ZSH-2117 is an NEDD4-recruiting EGFR PROTAC degrader. ZSH-2117 shows an IC50 of 13 nM against EGFRL858R/T790M/C797S, induces EGFR proteasome-dependent degradation, inhibits the downstream signaling pathways of EGFR, including the phosphorylation of AKT and ERK, suppresses cancer cell proliferation, and exhibits in vivo anti-tumor activity. ZSH-2117 can be used in research related to non-small cell lung cancer.
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PROTAC IKKβ/NR4A1 degrader-1
0 ImagesCat. No.: HY-179112CAS No.: 2826215-20-5PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand (HY-13067); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-79577).
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PROTAC HSP70 Degrader-1
0 ImagesCat. No.: HY-181147PROTAC HSP70 Degrader-1 (compound C4) is a cytosolic HSP70 PROTAC degrader that can engage CRBN to form a ternary complex. PROTAC HSP70 Degrader-1 mediates ubiquitination and proteasomal degradation of cytosolic HSP70. PROTAC HSP70 Degrader-1 exhibits cytotoxic activity against cancer cells, suppressing tumor cell proliferation and inducing apoptosis in combination with DTHIB. PROTAC HSP70 Degrader-1 can be used for the research of colon cancer and leukemia.
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iRucaparib-TP3
0 ImagesCat. No.: HY-130645CAS No.: 2410557-01-4
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Cath-L-dBET1
0 ImagesCat. No.: HY-173257Cath-L-dBET1 is a PROTAC degrader targeting BRD4. Cath-L-dBET1 has an IC50 value of 2.8 μM in MDA-MB-231 cells. Cath-L-dBET1 can be activated by cathepsin L (Cath-L) and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study.
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BRD4 degrader-6
0 ImagesCat. No.: HY-173327CAS No.: 3055207-38-7BRD4 degrader-6 is a dimeric BDR4 PROTAC degrader (DC50: < 0.1 μM). BRD4 degrader-6 promotes the ubiquitination and degradation of BDR4 and has anticancer activity.
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PROTAC HDAC8 Degrader-4
0 ImagesCat. No.: HY-181024PROTAC HDAC8 Degrader-3 (Compound BP6) is an efficient, selective and low-toxicity HDAC8 PROTAC degrader with a DC50 of 80 nM. PROTAC HDAC8 Degrader-3 exhibits IC50 of PROTAC for HDAC8 and CRBN of 0.26 and 30 μM respectively. PROTAC HDAC8 Degrader-3 increases the level of Ac-SMC3, stabilizes p53 and sensitizes targeted reagents (such as Idasanutlin (HY-15676)), demonstrating its great potential in combination therapy.
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PROTAC sEH degrader-3
0 ImagesCat. No.: HY-175392CAS No.: 3093413-94-3PROTAC sEH-degrader-3 is an sEH PROTAC degrader with an IC50 value of 5.5 nM against mouse sEH. PROTAC sEH-degrader-3 selectively degrades sEH in the cytoplasm but not in peroxisomes. PROTAC sEH-degrader-3 alleviates endoplasmic reticulum stress and acts as a cytoprotective agent. PROTAC sEH-degrader-3 can serve as a chemical probe for investigating the biological functions of sEH.
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MS99-β-Gal
0 ImagesCat. No.: HY-177945CAS No.: 3055593-63-7Synonyms: Gal-MS99MS99-β-Gal (Gal-MS99) is a galactose-modified NPM-ALK PROTAC degrader. MS99-β-Gal is only hydrolyzed by SA-β-gal and esterase in senescent cancer cells, releasing MS99, which specifically degrades the NPM-ALK fusion protein. MS99-β-Gal shows an IC50 of 454.8 nM for aging Karpas 299 cells, significantly lower than that of normal Karpas 299 cells (IC50 = 2.162 μM). MS99-β-Gal can be used for the research of cancer.
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NTLiverTac PDE6D degrader-1
0 ImagesCat. No.: HY-174379NTLiverTac PDE6D degrader-1 is a PDE6D NTLiverTac degrader with a DC50 of 4.09 μM. NTLiverTac PDE6D degrader-1 is formed by conjugating a PDE6D PROTAC degrader with the NTCP ligand Cholic acid (HY-N0324). NTLiverTac PDE6D degrader-1 triggers the ubiquitin-proteasome system-mediated degradation process by forming a complex with PDE6D and MDM2, inducing proteasome-dependent and NTCP-dependent degradation. NTLiverTac PDE6D degrader-1 inhibits PDE6D-dependent KRAS trafficking and suppresses KRAS-related oncogenic signaling cascades. NTLiverTac PDE6D degrader-1 inhibits the activation of the PI3K/AKT/mTOR signaling pathway and induces cellular Apoptosis. NTLiverTac PDE6D degrader-1 enters cancer cells via NTCP-mediated endocytosis. NTLiverTac PDE6D degrader-1 can be used in the research of hepatoblastoma (MDM2 ligand: (4R,5S)-Nutlin carboxylic acid (HY-128836); NTCP ligand: Cholic acid (HY-N0324); PDE6D ligand: Sorafenib (HY-10201)).
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PROTAC PIN1 degrader-2
0 ImagesCat. No.: HY-186218CAS No.: 3083422-10-7PROTAC PIN1 degrader-2 is a PROTAC PIN1 degrader. PROTAC PIN1 degrader-2 reduces PIN1-mediated oncogene expression, upregulates PIN1-inhibited tumor suppressor genes, and exerts killing effects on cancer cells. PROTAC PIN1 degrader-2 inhibits tumor growth in breast cancer mouse xenograft models. PROTAC PIN1 degrader-2 can be used for the research of breast cancer.
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SJH1-51B
0 ImagesCat. No.: HY-162240SJH1-51B is a SKP1-recruiting BRD4 PROTAC degrader. SJH1-51B binds to SKP1 in the SKP1-FBXO7-CUL1-RBX1 complex, but shows no or weak binding to monomeric SKP1. SJH1-51B induces proteasome- and SKP1-dependent degradation of BRD4, and this degradation process relies on the neddylation modification of Cullin-RING E3 ligase. SJH1-51B induces proteasome-mediated degradation of the short isoform of BRD4 in non-cancer cells, while it induces proteasome-mediated degradation of both the long and short isoforms of BRD4 in breast cancer cells. SJH1-51B can be used for breast cancer research.
