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 Produits associés (1355)
Produits associés (1355)
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Anticorps (1)
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PROTACs Isoform Comparison
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MS105
0 ImagesSynonyms: YX39-105MS105 (YX39-105) is an orally active and selective protein tyrosine kinase 6 (PTK6) (BRK) PROTAC degrader. MS105 recruits VHL E3 ligase via a VHL ligand moiety, promotes PTK6 ubiquitination and proteasomal degradation, inhibits the proliferation and migration of breast cancer cells, and induces apoptosis. MS105 shows potential for use in breast cancer research.
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SIAIS039
0 ImagesSIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker).
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MS15 TFA
0 ImagesCat. No.: HY-151613APureté: 99.82%
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PROTAC SMARCA2 degrader-8
0 ImagesPROTAC SMARCA2 degrader-8 is a SMARCA2 PROTAC degrader with a DC50 of 28 nM in A375 cells. PROTAC SMARCA2 degrader-8 forms a crystallizable ternary complex with the SMARCA4 bromodomain and VBC, promoting the ubiquitination and proteasomal degradation of SMARCA2. PROTAC SMARCA2 degrader-8 can be used in melanoma research.
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PROTAC CDK9 degrader-9
0 ImagesPROTAC CDK9 degrader-9 is an orally active, selective CDK9 PROTAC degrader with a DC50 of 3.94 nM. PROTAC CDK9 degrader-9 downregulates downstream targets c-Myc and MCL-1. PROTAC CDK9 degrader-9 inhibits the proliferation of breast cancer cells. PROTAC CDK9 degrader-9 can be used for the research of triple-negative breast cancer.
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PROTAC ATM degrader-1
0 ImagesPROTAC ATM degrader-1 is a ATM PROTAC degrader with a KD value of 1.17 nM. PROTAC ATM degrader-1 triggers DNA damage response, cell cycle arrest, and apoptosis in cancer cells via the ubiquitin-proteasome-dependent degradation pathway. PROTAC ATM degrader-1 can be used for research on colorectal cancer.
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AZ'6421
0 ImagesAZ'6421 is an orally active ERα PROTAC degrader with a DC50 of 0.4 nM. AZ'6421 recruits the VHL E3 ligase to form a ternary complex, inducing proteasome-mediated polyubiquitination and degradation of ERα. AZ'6421 inhibits the growth of ER+ cancer cells. AZ'6421 can be used in studies related to ER+ breast cancer.
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PROTAC EGFR degrader 8
0 ImagesPROTAC EGFR degrader 8 (T-184) is a PROTAC degrader that targets EGFR for degradation by recruiting cereblon. It induces EGFR protein degradation with a DC50 of 10.18 nM. The IC50 values of PROTAC EGFR degrader 8 for inhibiting the growth of H1975, PC-9 and HCC827 cells are 7.72, 121.9 and 14.21 nM, respectively. PROTAC EGFR degrader 8 inhibits the proliferation of EGFR-mutant non-small cell lung cancer cells and can be used in studies related to non-small cell lung cancer.
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PROTAC SARS-CoV-2 3CLPro degrader 2
0 ImagesCat. No.: HY-161177Pureté: 98.59%PROTAC KRAS G12D degrader 2 is a peptidomimetic PROTAC specifically targeting the dimeric SARS-CoV-2 3CLPro protein. PROTAC KRAS G12D degrader 2 inhibits SARS-CoV-2 3CLPro with an IC50 of 21.2 μM. PROTAC KRAS G12D degrader 2 specifically binds to the active site of SARS-CoV-2 3CLPro. PROTAC KRAS G12D degrader 2 reduces protein levels of SARS-CoV-2 3CLPro without affecting cell viability. PROTAC KRAS G12D degrader 2 can be used for the study of viral infections in Coronavirus genera.
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PROTAC HPK1 Degrader-1
0 ImagesPROTAC HPK1 Degrader-1 (compound B1) is a PROTAC degrader that recruits cereblon to induce HPK1 degradation, with a DC50 of 1.8 nM. PROTAC HPK1 Degrader-1 inhibits HPK1 kinase activity, with an IC50 of 140.5 nM. PROTAC HPK1 Degrader-1 suppresses the phosphorylation of SLP76 protein, with an IC50 of 496.1 nM. PROTAC HPK1 Degrader-1 can be used to investigate non-kinase-dependent signaling of HPK1 in the TCR pathway and cancer-related research.
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SP27
0 ImagesSP27 is a PROTAC PLK4 degrader with an IC50 of 8.4 nM and a DC50 of 19.5 nM against PLK4. SP27 induces PLK4 degradation via the CRBN-dependent ubiquitin-proteasome pathway, inhibits PLK4 downstream signal transduction, and suppresses the growth of TRIM37-amplified breast cancer cells. SP27 is applicable for breast cancer-related research.
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BR-cpd7
0 ImagesCat. No.: HY-163705Pureté: 98.01%BR-cpd7 is an orally active, selective PROTAC degrader targeting FGFR1 and FGFR2, with a DC50 of 2.2 nM against FGFR1. BR-cpd7 reduces FGFR signaling. BR-cpd7 induces cell cycle arrest and selectively blocks the proliferation of FGFR1/FGFR2-dependent tumor cells. BR-cpd7 exhibits significant antitumor efficacy in FGFR1-dependent lung cancer animal models, while achieving complete depletion of FGFR1. BR-cpd7 can be used for cancer-related research.
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G9D-4 TFA
0 ImagesCat. No.: HY-162749APureté: 99.44%G9D-4 TFA is a G9a PROTAC degrader. G9D-4 TFA induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 TFA exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 TFA can be used for research on pancreatic cancer.
