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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
44 Results for "
H3K4me
" in MedChemExpress (MCE) Product Catalog:
Products (44)
44 Results for "H3K4me" in MCE Product Catalog:
14
14 Publications Verification
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CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
14
14 Publications Verification
Cat. No.: HY-100421A
CAS No.: 2095432-28-1
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CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
8
8 Cited Publications
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KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels .
7
7 Cited Publications
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A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
5
5 Cited Publications
Cat. No.: HY-16705
CAS No.: 1374601-40-7
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BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 μM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence .
5
5 Cited Publications
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KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B) .
3
3 Cited Publications
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MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells .
2
2 Cited Publications
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CBB1007 trihydrochloride is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 trihydrochloride significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 trihydrochloride shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 trihydrochloride is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma .
1
1 Cited Publications
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YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. YUKA1 has less inhibitory active on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 can increase H3K4me3 levels and inhibit cell proliferation. YUKA1 can be used for the research of cancer, such as lung and breast cancers .
1
1 Cited Publications
Cat. No.: HY-N0857
CAS No.: 79233-15-1
1
Cat. No.: HY-403538
CAS No.: 1358901-59-3
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iZMYND8-34 is a ZMYND8 inhibitor with an IC50 of 0.66 μM. iZMYND8-34 inhibits the binding of H3K4me1–H3K14ac peptide to the ZMYND8 protein. iZMYND8-34 inhibits ZMYND8’s histone recognition. iZMYND8-34 blocks neuroendocrine prostate cancer development .
Cat. No.: HY-P2255
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Synonyms: JADA82 trihydrochloride; PCK82 trihydrochloride
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JQKD82 (JADA82) trihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 trihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma .
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KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs .
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GT-653 is a selective KDM5B PROTAC degrader. GT-653 induces ubiquitination and degradation of KDM5B without altering the transcriptional level of KDM5B. GT-653 upregulates the level of H3K4me3. GT-653 activates the type I Interferon signaling pathway. GT-653 can be used for the research of prostate cancer .
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Cat. No.: HY-138691
CAS No.: 2410512-38-6
Synonyms: JADA82; PCK82
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JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma .
Cat. No.: HY-P2257
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Cat. No.: HY-150619
CAS No.: 2230475-63-3
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KDM4-IN-4 (compound 47) is a potent histone lysine demethylase 4 (KDM4) inhibitor with a modest affinity binding to ~80 μM for KDM4A-Tudor domain. KDM4-IN-4 can inhibit H3K4Me3 binding to the Tudor domain in cells with an EC50 value of 105 μM. KDM4-IN-4 can be used for researching anticancer .
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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
