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 (1355)
Related Products (1355)
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Antibodies (1)
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PROTACs Isoform Comparison
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MS4077
0 ImagesMS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 37 nM for binding affinity to ALK.
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MS9427 TFA
0 ImagesCat. No.: HY-147941APurity: 98.38%MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer.
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YX-02-030
0 ImagesYX-02-030 is a VHL-dependent MDM2 PROTAC degrader with a Kd of 35 nM. YX-02-030 recruits the VHL E3 ligase to form a ternary complex, leading to ubiquitination and proteasome-mediated degradation of MDM2. YX-02-030 inhibits MDM2-p53 and VHL-HIF1α binding with IC50 values of 63 and 1350 nM. YX-02-030 activates TAp73, upregulates p53 family target genes and induces apoptosis. YX-02-030 demonstrates on-target efficacy in TNBC xenograft-bearing mice, extending survival without normal cell toxicity.
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AH078
0 ImagesAH078 is a PROTAC-based CK1δ/ε degrader (DC50=0.55 μM, Dmax=70%) that lacks subtype selectivity between CK1δ and CK1ε. AH078 induces target protein degradation either by recruiting the CUL4-CRBN E3 ligase complex and proteasome, or via the VHL- and ubiquitin-dependent pathway. AH078 also exhibits selectivity for CK1α, and is widely applicable to research related to colon cancer, pancreatic cancer, breast cancer, ovarian cancer, chronic lymphocytic leukemia, acute myeloid leukemia, glioma, and metastatic breast adenocarcinoma.
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PROTAC ERα Degrader-4
0 ImagesPROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
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PROTAC EGFR degrader 2
0 ImagesCat. No.: HY-144304CAS No.: 3031336-58-7
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SB1-G-187
0 ImagesSB1-G-187 is a multi-target kinase PROTAC degrader with activity against various kinases including GCK, YES1, IRAK1 and LYN. SB1-G-187 induces degradation of target kinases via a p97-dependent pathway, and forms ternary complexes with CRBN and specific functional kinases. SB1-G-187 can be used in tumor-related research.
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KTX-951
0 ImagesKTX-951 is an orally active PROTAC degrader of IRAK4 and IMiD (Ikaros/Aiolos) substrates (Kd = 3.5 nM). KTX-951 induces IRAK4 degradation, and the degradation efficiency is independent of IRAK4 binding affinity. The DC50 values of KTX-951 for IRAK4, Ikaros and Aiolos are 18 nM, 14 nM and 13 nM, respectively. The IC50 of KTX-951 against OCl-Ly10 CTG is 35 nM. KTX-951 exhibits antitumor activity.
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PROTAC MNK1 degrader-1
0 ImagesSynonyms: P11-2PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM, and a Dmax > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC50: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety.
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dAURK-4 hydrochloride
0 ImagesCat. No.: HY-137344APurity: 98.14%dAURK-4 hydrochloride is a selective AURKA PROTAC degrader. dAURK-4 hydrochloride promotes ubiquitination and degradation of AURKA. dAURK-4 hydrochloride can be used in the research of glioblastoma and multiple myeloma.
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PROTAC HDAC6 degrader 11
0 ImagesPROTAC HDAC6 degrader 11 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. PROTAC HDAC6 degrader 11 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. PROTAC HDAC6 degrader 11 causes strong hyperacetylation of α-tubulin.
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HD-TAC7
0 ImagesHD-TAC7 is a potent PROTAC HDAC degrader with IC50 values of 3.6 μM, 4.2 μM and 1.1 μM for HDAC1, HDAC2 and HDAC3, respectively. HD-TAC7 can decreases NF-κB p65 in RAW 264.7 macrophages. HD-TAC7 can be used for the research of inflammatory diseases like asthma and chronic obstructive pulmonary disease (COPD).
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RSS0680
0 ImagesRSS0680 is a small noncoding RNA (sRNA) targeting the mRNA ribosome binding site (RBS) and a PROTAC. RSS0680 competitively binds to RBS through the conserved CCUCCUCCC anti-Shine-Dalgarno (aSD) sequence and inhibits the translation initiation of target genes. RSS0680 can interact with the DUF1127 protein CcaF1, regulate its own stability and participate in bacterial oxidative stress defense, enhancing the host's resistance to heat shock and oxidative damage by affecting pathways such as C1 metabolism and pyruvate dehydrogenase complex. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used to study diseases or disorders mediated by aberrant kinase activity and regulatory mechanisms of noncoding RNAs in α-proteobacteria[1][2].
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PROTAC HIF-1α degrader-1
0 ImagesCat. No.: HY-168641Purity: 98.02%PROTAC HIF-1α degrader-1 is a potent HIF-1α PROTAC degrader. PROTAC HIF-1α degrader-1 induces ubiquitination and degradation of HIF-1α protein under hypoxic conditions. PROTAC HIF-1α degrader-1 induces Apoptosis. PROTAC HIF-1α degrader-1 can be used for the research of breast cancer and hepatocellular carcinoma.
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CG428
0 ImagesCG428 is a potent and selective CRBN-dependent tropomyosin receptor kinase (TRK) PROTAC degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1 phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). CG428 can be used for the research of colorectal carcinoma.
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WZS0347
0 ImagesCat. No.: HY-179717Purity: 99.06%WZS0347 is a MITF PROTAC degrader. WZS0347 effectively reduces the MITF protein levels in several melanoma cell lines, including B16F10, A375, and GAK. WZS0347 significantly inhibits the proliferation, migration, and invasion of melanoma cells. WZS0347 can be used for research on melanoma.
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MS9449
0 ImagesMS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer.
