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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
21 Results for "
EOL-1
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "EOL-1" in MCE Product Catalog:
3
3 Cited Publications
Research Areas:
MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12 nM). MS177 effectively depletes both canonical EZH2-PRC2 and noncanonical EZH2-cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest [1].
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2 Cited Publications
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VZ185 is a BRD9 and BRD7 PROTAC degrader, with DC50 values of 1.76 nM and 4.5 nM, respectively, in RI-1 cells; and DC50 values of 4 nM and 34 nM, respectively, in HEK293 cells. VZ185 hijacks the CRL2 VHL E3 ubiquitin ligase complex to induce ubiquitination and subsequent proteasomal degradation of BRD9 and BRD7. VZ185 can be used in research related to acute myeloid eosinophilic leukemia and malignant rhabdoid tumors [1].
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1 Cited Publications
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GNE-987 is a VHL-dependent BRD4 PROTAC degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 can be used for the research of cancer [1].
1
1 Cited Publications
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dBRD9 is a BRD9 PROTAC degrader. dBRD9 reduces the binding of the ISGF3 complex to ISG promoters, decreases the level of ISG induction downstream of IFNAR signaling, and reduces the chromatin binding of BRD4 at BRD9 co-binding sites. dBRD9 can be used in research related to acute myeloid leukemia [1].
1
1 Cited Publications
Cat. No.: HY-117690A
CAS No.: 2341840-98-8
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dBRD9 dihydrochloride is a BRD9 PROTAC degrader. dBRD9 dihydrochloride reduces the binding of the ISGF3 complex to ISG promoters, decreases the level of ISG induction downstream of IFNAR signaling, and reduces the chromatin binding of BRD4 at BRD9 co-binding sites. dBRD9 dihydrochloride can be used in research related to acute myeloid leukemia [1].
Cat. No.: HY-162250
CAS No.: 3050872-59-5
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MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC50=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer [1].
Cat. No.: HY-155815
Purity: 97.60%
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MS9715 is a selective NSD3 PROTAC degrader with a Kd value of 1.3 μM and a DC50 of 4.9 μM. MS9715 recruits the VHL E3 ligase to mediate the ubiquitination and degradation of NSD3. MS9715 downregulates oncogenes including CBLB, IFITM1 and MAP7. MS9715 induces Apoptosis. MS9715 is applicable to the research of hematological malignancies and lung cancer [1] .
Cat. No.: HY-155529
CAS No.: 1422456-47-0
FD1024 is PIM inhibitor (IC50s: 1.96, 38.9, 4.17 nM for PIM1, 2, 3). FD1024 can be used for research of acute myeloid leukemia. FD1024 has strong antiproliferative activity against the tested AML cell lines, with 0.16 μM, 0.12 μM, 1.05 μM, 1.39μM for EOL-1, MV-4-11, KG-1, MOLM-16 cells. FD1024 also has antitumor efficacy in mice [1].
Cat. No.: HY-122130
CAS No.: 1146209-50-8
Synonyms: MK-8267
SCH 2047069 (MK-8267) is an orally active kinesin spindle protein (KSP) inhibitor (Kd: 0.5 nM) that can cross the blood-brain barrier. SCH 2047069 exhibits an IC50 value of ≤ 5 nM against the KSP ATPase. SCH 2047069 exhibits broad-spectrum antitumor activity. SCH 2047069 can induce mitotic arrest and apoptosis in tumor cells. SCH 2047069 can be used in the research of tumors such as ovarian cancer, colon cancer, glioblastoma, and lymphoma [1] .
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Thalidomide-NH-PEG2-C2-NH-Boc is a synthesized?E3 ligase ligand-linker conjugate?that incorporates the?Thalidomide?based cereblon ligand and a PEG linker used for dBRD9 (compound 6) synthesis. dBRD9 is a selective BRD9 probe PROTAC degrader for the study of BAF complex biology [1].
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Ki11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC50 values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis [1] .
Cat. No.: HY-P991641
Synonyms: LY3012218
Cat. No.: HY-138637
CAS No.: 3026420-43-6
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PROTAC BRD4 Degrader-14 is a PROTAC-type BRD4 degrader, which is predicted to be a weak VHL binder and an inactive BRD4 degrader [1].
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PROTAC BRD4 Degrader linker conjugate-2 is a PROTAC-based BRD4 degrader [1].
Cat. No.: HY-129937
CAS No.: 2738533-33-8
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(S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 can be used to design PROTAC-Antibody Conjugate (PAC) [1].
Cat. No.: HY-146680
CAS No.: 2278278-04-7
FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC50 of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research [1].
Cat. No.: HY-186269
CAS No.: 3050872-76-6
MS8847N1 is a negative control analog of MS8847 (HY-162250), which abolishes binding to EZH2 while retaining the activity of recruiting VHL. MS8847N1 does not induce EZH2 degradation. MS8847N1 can be used in PROTAC-related research [1].
Cat. No.: HY-181587
PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA, a Ki of 93.3 nM against CA IX, and a Ki of 80.0 nM against CA XII. PDGFRA/CAIX/XII-IN-1 binds to the ATP-binding pocket of PDGFRA and blocks the downstream STAT3, AKT and ERK1/2 signaling pathways. PDGFRA/CAIX/XII-IN-1 induces G0/G1 cell cycle arrest and endogenous apoptosis (Apoptosis), including cleavage of PARP-1, caspase-9 and caspase-3, activation of caspase 3/7, and down-regulation of Mcl-1. PDGFRA/CAIX/XII-IN-1 exhibits antiproliferative activity in eosinophilic leukemia cells. PDGFRA/CAIX/XII-IN-1 can be used for the research of leukemia [1].
Cat. No.: HY-186272
CAS No.: 3050872-64-2
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MS8847N2 is a negative control analog of an EZH2 PROTAC degrader that binds EZH2 but does not bind the VHL E3 ligase or induce EZH2 degradation [1].
Cat. No.: HY-181925
FD2024 is a pan-PIM kinase inhibitor with IC50 values of 0.17 nM, 1.86 nM, and 0.38 nM against PIM-1, PIM-2, and PIM-3, respectively. FD2024 induces cell apoptosis. FD2024 inhibits the phosphorylation of mTOR, p70S6K, S6, 4EBP1, and BAD proteins. FD2024 exhibits anti-acute myeloid leukemia activity. FD2024 can be used in studies related to acute myeloid leukemia [1].
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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
