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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
8320 Results for "
Protac
" in MedChemExpress (MCE) Product Catalog:
Products (8320)
8320 Results for "Protac" in MCE Product Catalog:
Cat. No.: HY-139620
CAS No.: 2762181-19-9
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MS83 is a selective degrader of BRD4/BRD3 belonging to the PROTAC class. MS83 hijacks the KEAP1-dependent CUL3 ligase complex by binding to KEAP1 and forming a ternary complex with BRD4/BRD3. MS83 induces polyubiquitination and degradation of BRD4/BRD3 in a concentration-, time- and ubiquitin-proteasome system-dependent manner. MS83 inhibits c-MYC protein levels and suppresses the proliferation of triple-negative breast cancer cells .
Cat. No.: HY-143883
CAS No.: 2376137-41-4
MS143 is a VHL-recruiting AKT protein PROTAC degrader with a DC50 of 46 nM in PC3 prostate cancer cells. MS143 preferentially binds to AKT1 and AKT3, with weaker binding activity towards AKT2. MS143 degrades AKT and blocks the phosphorylation of downstream signaling molecules in the PI3K/AKT/mTOR pathway. MS143 inhibits cancer cell growth and xenograft tumor growth. MS143 can be used for research on prostate cancer, triple-negative breast cancer, and breast cancer .
Cat. No.: HY-145281
CAS No.: 2376137-31-2
MS98 is a AKT PROTAC degrader with a DC50 of 78 nM in BT474 cells. MS98 binds to purified AKT1, AKT2 and AKT3 isoforms with Kd values of 4 nM, 140 nM and 8 nM, respectively. MS98 recruits the VHL E3 ligase to induce polyubiquitination and proteasomal degradation of AKT. MS98 inhibits downstream signal transduction of the PI3K/AKT/m-TOR pathway. MS98 suppresses cancer cell proliferation. MS98 can be used for the research of prostate cancer and breast cancer .
Cat. No.: HY-146231A
Purity: 99.88%
SS47 TFA is a hematopoietic progenitor kinase HPK1 PROTAC-class degrader and immune activator. SS47 TFA promotes the proliferation of CD4+ and CD8+ T cells as well as IFN-γ secretion, and enhances the anti-tumor cytotoxicity and in vivo efficacy of BCMA CAR-T cells. SS47 TFA also inhibits tumor growth in mouse models, and when combined with anti-PD-1 therapy, it improves the immune response of 4T1 tumor-bearing mice. SS47 TFA can be used in breast cancer-related research .
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HD-TAC7 is a selective HDAC3 PROTAC degrader with an IC50 of 1.1 μM. By recruiting the CRBN E3 ligase, HD-TAC7 induces ubiquitin-proteasome degradation and selective downregulation of HDAC3, which in turn increases H3K27 acetylation levels and downregulates the NF-κB subunit p65, exerting anti-inflammatory activity. HD-TAC7 is used in research on COVID-19, SARS-CoV-2 infection, asthma, chronic obstructive pulmonary disease, and colon cancer .
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MS8815 is a EZH2 PROTAC degrader, with a DC50 of 140 nM in MDA-MB-453 triple-negative breast cancer (TNBC) cells and an IC50 of 8.6 nM against human EZH2. MS8815 induces ubiquitin-proteasome system-mediated degradation of EZH2, reduces the levels of EED, SUZ12, FOXM1, H3K27me3 and global m6A, and increases the protein level of HMGCS2. MS8815 can be used in the research of breast cancer and prostate cancer .
Cat. No.: HY-153573
Synonyms: dCym-JQ1
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SRG-II-19F (dCym-JQ1) is a BRDTBD1 PROTAC degrader. Its dCym moiety at one end binds to the N-terminal domain of ClpC1 (ClpC1NTD), while its JQ1 moiety at the other end binds to bromodomain 1 of BRDT (BRDTBD1). This molecule induces the degradation of BRDTBD1 by recruiting the BRDTBD1 substrate to the ClpC1P1P2 protease complex. SRG-II-19F serves as a research tool for studies related to mycobacterial protein degradation .
Cat. No.: HY-157559
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KDRLKZ-2 is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 95 nM), with an IC50 of 68 nM and 0.1 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-2 binds to the substrate-binding pocket of the kelch domain of KLHDC2, mimics the interaction of natural substrates and displaces them. KDRLKZ-2 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-2 can be used in scaffold ligand studies of PROTAC degraders targeting KLHDC2 .
Cat. No.: HY-161131
CAS No.: 2399455-71-9
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Lenalidomide 4'-alkyl-C3-azide (compound 4a) is a click chemical modified Lenalidomide (HY-A0003) that can be used to synthesize PROTACs. Lenalidomide is an orally active immunomodulator and a ligand for the ubiquitin E3 ligase cereblon (CRBN). Lenalidomide 4'-alkyl-C3-azide contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition reactions (SPAAC) can also occur with molecules containing DBCO or BCN groups .
Cat. No.: HY-161197
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Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
Cat. No.: HY-161710
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XYD129 is a CBP/p300 PROTAC degrader. XYD129 potently binds to CBP, p300 and CRBN proteins, with IC50 values of 0.021 μM, 0.03 μM and 0.18 μM, respectively. XYD129 forms a ternary CRBN-CBP/p300 complex and induces CBP/p300 degradation via the ubiquitin-proteasome system. XYD129 inhibits tumor growth and suppresses the proliferation of acute myeloid leukemia cells. XYD129 can be used in studies related to acute myeloid leukemia .
Cat. No.: HY-162538
CAS No.: 3053823-69-8
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LC-MI-3 is an orally active IRAK4 PROTAC degrader with an IC50 of 57.2 nM and high selectivity among human protein kinases. LC-MI-3 eliminates IRAK4 kinase and scaffolding functions via the cereblon E3 ubiquitin ligase and ubiquitin-proteasome systems. LC-MI-3 inhibits downstream nuclear factor-κB and IRAK4-mediated inflammatory signaling pathways. LC-MI-3 can be used for the research of acute lung injury, sepsis, psoriasis, and inflammatory diseases .
Cat. No.: HY-163168
CAS No.: 2412985-00-1
Synonyms: CFT-4531
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aTAG 4531 (CFT-4531) is a PROTAC-class degrader that induces the degradation of the MTH1/aTAG fusion protein by recruiting cereblon, with a DC50 of 0.28 nM in Jurkat cells. aTAG 4531 inhibits MTH1 enzymatic activity, with a Ki of 1.8 nM. aTAG 4531 rapidly, selectively and reversibly regulates SMART-CAR protein levels, CAR-mediated target cell killing and IL-2 release, and is applicable both in vitro and in vivo. aTAG 4531 can be used in studies of targeted protein degradation, target validation and CAR-T activity regulation .
Cat. No.: HY-163220
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(S,R,S)-AHPC-CO-CH2-O-CH2-piperidine-Boc is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. (S,R,S)-AHPC-CO-CH2-O-CH2-piperidine-Boc can be used as a key intermediate for the synthesis of complete PROTAC molecules.
Cat. No.: HY-163223
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(S,R,S)-AHPC-CO-CH2-piperazine-C3-piperazine-Boc is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. (S,R,S)-AHPC-CO-CH2-piperazine-C3-piperazine-Boc can be used as a key intermediate for the synthesis of complete PROTAC molecules.
Cat. No.: HY-163231
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(S,R,S)-AHPC-CO-CH2-azetidine-piperazine-CH2-COOH is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. (S,R,S)-AHPC-CO-CH2-azetidine-piperazine-CH2-COOH can be used as a key intermediate for the synthesis of complete PROTAC molecules.
Cat. No.: HY-168026
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CEP1347-VHL-02 is a selective MLK3 PROTAC degrader that mediates MLK3 degradation via the ubiquitin-proteasome system, with a DC50 of 50-300 nM. After degrading MLK3, CEP1347-VHL-02 inhibits downstream JNK signaling, induces G2/M phase arrest and apoptosis in cancer cells, and suppresses their clonogenic, migratory and 3D sphere-forming abilities. CEP1347-VHL-02 can be used for the research of triple-negative breast cancer .
Cat. No.: HY-168556
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YJ9069 is a CDK12/CDK13 PROTAC degrader. YJ9069 induces proteasome-dependent degradation of CDK12 and CDK13, and inhibits serine 2 phosphorylation of RNA polymerase II (RNA polymerase II). YJ9069 triggers gene length-dependent transcription elongation defects, reduces the expression of DNA damage response genes, and induces DNA damage, cell cycle arrest and apoptosis. YJ9069 inhibits tumor growth in prostate cancer models. YJ9069 can be used for the research of prostate cancer, Ewing sarcoma and breast cancer .
Cat. No.: HY-168634
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SJ46421 is a BRD3BD2 PROTAC degrader. SJ46421 induces a cooperative ternary complex of KLHDC2 and BRD3BD2 with an IC50 of 7.8 nM. SJ46421 binds to the substrate-binding pocket of KLHDC2, forms cooperative ternary complexes with BRD3BD2, BRD2BD2 and BRD4BD2, disrupts the autoinhibitory tetramer assembly of KLHDC2, drives selective ubiquitination of BRD3BD2, and inhibits the ubiquitination of endogenous KLHDC2 diglycine substrates. SJ46421 can be used in cancer research .
Cat. No.: HY-169133
CAS No.: 2991588-80-6
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GDCNF-11 is a type of HSP90 interaction-mediated protein degradation chimera (HIM-PROTAC) degrader that targets and degrades GPX4, with a DC50 of 0.08 μM. GDCNF-11 mediates the ubiquitination and proteasome-dependent degradation of GPX4 by recruiting GPX4 to form a ternary complex with HSP90, increases intracellular lipid peroxides and ROS, and ultimately triggers Ferroptosis. GDCNF-11 inhibits tumor growth in mouse models, downregulates GPX4 protein in xenograft tumors, and upregulates the lipid peroxidation marker. GDCNF-11 can be used for the research of fibrosarcoma .
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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
