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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
27 Results for "
PROTAC mechanism
" in MedChemExpress (MCE) Product Catalog:
Products (27)
27 Results for "PROTAC mechanism" in MCE Product Catalog:
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1 Cited Publications
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AD4 is a PROTAC that induces the degradation of PCLAF by recruiting cereblon. AD4 is also an artemisinin derivative. AD4 directly binds to PCLAF with a KD of 6.1 μM, and induces apoptosis and G1-phase cell cycle arrest. By degrading PCLAF, AD4 upregulates p21, reduces Rb phosphorylation, downregulates Bcl-2 and upregulates Bax, thereby activating the p21/Rb axis. AD4 can be used in studies related to acute B-lymphoblastic leukemia and PCLAF-dependent anticancer mechanisms .
Cat. No.: HY-162362
CAS No.: 3060730-06-2
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MS8709 is a PROTAC degrader that induces the degradation of G9a (EHMT2)/GLP (EHMT1) by recruiting VHL. MS8709 induces G9a/GLP protein degradation via a mechanism that simultaneously depends on G9a/GLP target protein binding, VHL recruitment, and the ubiquitin-proteasome system (UPS), while the mRNA levels of G9a and GLP do not show significant changes, indicating that the effect occurs primarily at the protein level rather than the transcriptional level. MS8709 retains the inhibitory effect on G9a/GLP methyltransferase activity and reduces H3K9me2 levels, thereby simultaneously affecting the catalytic and non-catalytic functions of G9a/GLP. MS8709 can be used for studies related to G9a/GLP biology, prostate cancer, lung cancer, and other relevant fields .
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PROTACs CDK AAK1 Cyclin G-associated Kinase (GAK) Salt-inducible Kinase (SIK) LIM Kinase (LIMK) Wee1 SnRK
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RSS0680 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].
Cat. No.: HY-156373
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MN714 is a prodrug of MN551 (HY-156395) with enhanced cell permeability. MN714 specifically and covalently binds to SOCS2 within living cells, with an EC50 of 3.77 μM at 2 h and 2.52 μM at 8 h. MN714 serves as a chemical probe for investigating the biological mechanisms of the SOCS2 and CRL5 complex, and also functions as an E3 ligase linker for PROTAC development .
Cat. No.: HY-179433
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PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .
Cat. No.: HY-175417
VHL-SNAP2-5C is a PROTAC degrader targeting SNAP-tag fusion proteins, with an IC50 of 0.33 μM for binding to VHL. VHL-SNAP2-5C covalently binds to the SNAP-tag target at one end and recruits the VHL ubiquitin E3 ligase at the other end to form a ternary complex, thereby inducing proteasome-dependent ubiquitination and degradation of SNAP fusion proteins through its heterobifunctional structure. VHL-SNAP2-5C can be used in studies of protein homeostasis and degradation mechanisms .
Cat. No.: HY-178122
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THNAN69 is a PROTAC degrader targeting LIMK2, which efficiently degrades ectopically expressed EGFP-LIMK2 in live HuCCT1 cells with a DC50 of 1 nM. THNAN69 induces isoform-specific ubiquitin-mediated degradation of LIMK2 by recruiting the CRBN E3 ligase, forming a stable ternary complex with LIMK2 and CRBN; this degradation process depends on the activity of cullin-RING ligase. THNAN69 does not reduce phosphorylated cofilin levels, as LIMK1 can compensate for the loss of LIMK2; it also stimulates compensatory activation of the Rho signaling pathway including PAK1/2 and ROCK1/2. THNAN69 serves as a selective chemical probe for dissecting the LIMK2 isoform-dependent biological mechanisms. THNAN69 can be used in the research of cholangiocellular carcinoma and acute lymphoblastic leukemia .
Cat. No.: HY-163811
CAS No.: 3024541-39-4
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BRD9 Degrader-4 is a bifunctional targeted degrader of the BRD9 protein, which promotes proteasomal degradation of BRD9 via a non-canonical PROTAC mechanism independent of the CRBN or VHL E3 ligases .
Cat. No.: HY-179424
CAS No.: 3095636-64-6
PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. PROTAC HIF-1α degrader-2 inhibits HeLa cell proliferation, migration, and colony formation, and induces apoptosis. PROTAC HIF-1α degrader-2 reduces p-MEK and p-AKT expression in the MAPK and PI3K/AKT pathways. PROTAC HIF-1α degrader-2 can be used for the study of cervical cancer .
Cat. No.: HY-179434
CAS No.: 3095636-66-8
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HIF-1α-IN-10 is a ligands for target protein for PROTAC (HIF-1α). HIF-1α-IN-10 can be used to synthesize PROTAC HIF-1α degrader-2 (HY-179424) .
Cat. No.: HY-172144
CAS No.: 3038446-90-8
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JB300 is a PROTAC degrader that selectively targets and degrades AURORA-A by recruiting cereblon, with EC50 values of 373 nM and 193 nM in intact cells and permeabilized cells, respectively. JB300 can be used in studies related to acute myeloid leukemia and targeted protein degradation mechanisms .
Cat. No.: HY-161708
CAS No.: 3075001-08-7
PROTAC FLT3/CDKs degrader-1 is a PROTAC degrader targeting CDKs and FLT3. PROTAC FLT3/CDKs degrader-1 degrades CDK2, CDK4, CDK6, CDK9 and FLT3 proteins via a ubiquitin-proteasome-dependent bivalent mechanism, with a DC50 of 18.73 nM against CDK2. PROTAC FLT3/CDKs degrader-1 promotes myeloid cell differentiation. PROTAC FLT3/CDKs degrader-1 inhibits leukemia cell proliferation. PROTAC FLT3/CDKs degrader-1 can be used for the research of acute myeloid leukemia .
Cat. No.: HY-163810
CAS No.: 3033018-77-5
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BRD9 Degrader-3 is a selective BRD9 BRD9 molecular glue degrader degrader. BRD9 Degrader-3 consists of a BRD9-binding ligand, a linker, and a warhead that promotes proteasomal degradation of BRD9 via a non-canonical PROTAC mechanism independent of CRBN or VHL E3 ligases. BRD9 Degrader-3 can be used in cancer research, including studies of malignant rhabdoid tumors, specific sarcomas, and acute myeloid leukemia .
Cat. No.: HY-163809
CAS No.: 3033018-68-4
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BRD9 Degrader-2 is a selective BRD9 molecular glue degrader. BRD9 Degrader-2 consists of a BRD9-binding ligand, a linker, and a warhead that promotes proteasomal degradation of BRD9 via a non-canonical PROTAC mechanism independent of CRBN or VHL E3 ligases. BRD9 Degrader-2 can be used in cancer research, including studies of malignant rhabdoid tumors, specific sarcomas, and acute myeloid leukemia .
Cat. No.: HY-163813
CAS No.: 3023359-76-1
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AR Degrader-2 is a bifunctional androgen receptor degrader that is applicable to cancer-related research .
Cat. No.: HY-174248
PS21M is a negative control PROTAC degrader derived from CPS-021, as well as an inhibitor of ternary complex formation. PS21M attenuates the interaction with Cereblon ligase, restricting the formation of the PAK4-PROTAC-Cereblon ternary complex and the subsequent degradation of PAK4. PS21M serves as a negative control molecule to verify the degradation mechanism of CPS-021 .
Cat. No.: HY-179435
CAS No.: 2408342-03-8
Synonyms: VH032-NH-Bromooctanoic acid
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(S,R,S)-AHPC-Bromooctanoic acid is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding linker (HY-W007700). (S,R,S)-AHPC-Bromooctanoic acid can serve as VHL (von Hippel-Lindau) ligand to recruit the VHL protein and serve as a key intermediate for the synthesis of complete PROTAC molecules .
Cat. No.: HY-180262
PROTAC CDK6 Degrader 2 (compound 48b), the active form of PROTAC CDK6 Degrader 1 (HY-180277), is a potent and selective PROTAC CDK6 degrader that binds strongly to KLHDC2 (KD = 0.005 μM). PROTAC CDK6 Degrader 2 functions through a KLHDC2-dependent and ubiquitin-proteasome-mediated mechanism. PROTAC CDK6 Degrader 2 can be used for cancer research .
Cat. No.: HY-183251
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PROTAC p300 degrader-1 is a paralog-selective, PROTAC-based degrader targeting the p300/CBP protein. It exhibits potent antiproliferative, cell cycle arrest and pro-apoptotic activities, and can be used in the research and development of antitumor drugs and related mechanism studies for hematological malignancies (AML, MM, NHL) .
Cat. No.: HY-181413
CAS No.: 3093642-25-9
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PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
