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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
28 Results for "
H1 histone
" in MedChemExpress (MCE) Product Catalog:
Products (28)
28 Results for "H1 histone" in MCE Product Catalog:
27
27 Publications Verification
Target:
Research Areas:
BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells .
27
27 Publications Verification
Cat. No.: HY-108239
CAS No.: 1392399-03-9
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BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells .
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12 Cited Publications
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A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity .
1
1 Cited Publications
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BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1 .
1
1 Cited Publications
Cat. No.: HY-P74887
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: H1-0; H1.0, H1(0), H1-0; Prev. H1F0; histone H1.0; Prev. H1FV; histone H1'; H1.0; H1 histone Family, Member 0; H1 histone Family Member 0; H10; H1.0 Linker histone; histone H1(0)
Species:
Human
Source:
E. coli
Cat. No.: HY-NP155A
CAS No.: 1523001-32-2
Cat. No.: HY-P2480
CAS No.: 889112-06-5
Cat. No.: HY-W516880
CAS No.: 73736-50-2
Synonyms: O-Demethylastemizole
Research Areas:
Desmethylastemizole (O-Demethylastemizole) , a metabolite of Astemizole (HY-12532), is a β-hematin (βH) inhibitor. Desmethylastemizole has an antiplasmodium activity against P. falciparum with IC50 of 0.12, 0.11 and 0.06 μM for Pf3D7, PfDd2, and PfItG strains, respectively. Desmethylastemizole is also a Histamine H1 receptor antagonist. Desmethylastemizole significantly blocks hERG K + channels and also inhibits histone-lysine N-methyltransferase EZH2 activity. Desmethylastemizole can be used for long QT syndrome and malaria research .
Cat. No.: HY-P3745
CAS No.: 65189-70-0
Cat. No.: HY-125209A
CAS No.: 2253744-57-7
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TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC50 of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9 .TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis .TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells .TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells .TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay .TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) .TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells .TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells .TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines .TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer .
Cat. No.: HY-P1906
CAS No.: 1670273-47-8
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Cat. No.: HY-P990574
CAS No.: 340013-96-9
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Cat. No.: HY-P1906A
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Cat. No.: HY-123597
CAS No.: 15427-93-7
Synonyms: DDUG; NCI C04808
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NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
Cat. No.: HY-182246
CAS No.: 1301757-19-6
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MC2050 is a selective PARP-1 inhibitor with an IC50 of 119 nM. MC2050 functionally inhibits PARP-1 activity, including hyperactivation induced by oxidative stress, and reduces the poly (ADP-ribosyl) ation level of histone H1. MC2050 protects neuroblastoma cells from oxidative stress-mediated cell death induced by hydrogen peroxide. MC2050 is applicable to research related to neuroblastoma and Burkitt lymphoma .
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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
