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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WZS0347
0 ImagesCat. No.: HY-179717Purity: 99.06%WZS0347 is a MITF PROTAC degrader. WZS0347 effectively reduces MITF protein levels in various melanoma cell lines. WZS0347 induces MITF degradation via the cereblon-dependent ubiquitin-proteasome pathway, downregulates the expression of downstream target genes of MITF, and inhibits the colony formation and migration abilities of cancer cells. WZS0347 can be used in melanoma-related research.
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MS9449
0 ImagesMS9449 is a potent PROTAC EGFR degrader, with Kd values of 17 nM and 10 nM for wild-type EGFR and mutant EGFRL858R, respectively, and a DC50 of 7.1 nM for EGFRDel19. MS9449 effectively induces the degradation of mutant EGFR through the ubiquitin-proteasome system (UPS) and the autophagy-lysosome pathway. MS9449 exhibits anticancer activity against non-small cell lung cancer. MS9449 can be applied in related research on non-small cell lung cancer.
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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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PROTAC RIPK degrader-6
0 ImagesPROTAC RIPK degrader-6 (Example 1) is a RIPK2 PROTAC degrader that recruits cereblon. PROTAC RIPK degrader-6 recruits the CRBN E3 ubiquitin ligase complex and induces the degradation of RIPK2 kinase via the ubiquitin-proteasome pathway, thereby blocking NOD1/NOD2-mediated pro-inflammatory signaling pathways of NF-κB and MAPK. PROTAC RIPK degrader-6 can be used in research related to RIPK2-mediated autoinflammatory diseases and cancer.
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MS15 TFA
0 ImagesCat. No.: HY-151613APurity: 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-161177Purity: 99.05%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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HL-8
0 ImagesHL-8 is a PI3Kα PROTAC degrader. HL-8 promotes the ubiquitination and degradation of PI3Kα. HL-8 reduces pAKT levels. HL-8 has anticancer activity against colon and cervical cancer (Pink: PI3Kα ligand (HY-143277); Blue: E3 ligase VHL ligand (HY-138678); Black: linker (HY-W002042)).
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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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XZ338
0 ImagesCat. No.: HY-172798Purity: 98.17%XZ338 is a highly potent and selective BCL-XL PROTAC degrader derived from A-1331852 (HY-19741), with a DC50 of 0.43 nM in MOLT‑4 cells. XZ338 induces the formation of a ternary complex with BCL-XL and VHL E3 ligase, mediates target protein degradation via the ubiquitin-proteasome system, and exhibits significantly weaker degradation activity in platelets than in tumor cells. XZ338 possesses anti-cancer activity. XZ338 can be used in the research of T-cell acute lymphoblastic leukemia (T-ALL).
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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.
