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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
17 Results for "
histone hyperacetylation
" in MedChemExpress (MCE) Product Catalog:
Products (17)
17 Results for "histone hyperacetylation" in MCE Product Catalog:
33
33 Cited Publications
Synonyms: Butanoic acid sodium; Butyric acid sodium
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1
1 Cited Publications
Cat. No.: HY-164233
CAS No.: 2742732-92-7
YX968 is a selective HDAC3/HDAC8 PROTAC dual degrader, with a DC50 value of 1.7 nM against HDAC3 and 6.1 nM against HDAC8. YX968 inhibits cancer cell growth, induces apoptosis, prevents global histone hyperacetylation, and exerts effects via antiproliferative activity. YX968 can be used in research related to triple-negative breast cancer, non-small cell lung cancer, and multiple myeloma .
Cat. No.: HY-171140
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PROTAC HDAC6 degrader 3 is a selective HDAC6 PROTAC degrader with an IC50 of 0.686 μM and shows high selectivity for HDAC6 over HDAC1-4. PROTAC HDAC6 degrader 3 recruits cereblon (CRBN) to trigger HDAC6 ubiquitination and subsequent proteasomal degradation. PROTAC HDAC6 degrader 3 selectively elevates acetylated α-tubulin levels in cancer cells, and does not induce histone H3 hyperacetylation or obvious loss of cell viability. PROTAC HDAC6 degrader 3 is applicable for research on multiple myeloma .
Cat. No.: HY-171139
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PROTAC HDAC6 degrader 2 is a non‑hydroxamate selective HDAC6 PROTAC degrader with an IC50 of 0.643 μM and shows high selectivity for HDAC6 over HDAC1-4. PROTAC HDAC6 degrader 2 recruits VHL E3 ubiquitin ligase to trigger HDAC6 ubiquitination and subsequent proteasomal degradation. PROTAC HDAC6 degrader 2 selectively elevates acetylated α-tubulin levels in cancer cells, and does not induce histone H3 hyperacetylation or obvious loss of cell viability. PROTAC HDAC6 degrader 2 is applicable for research on multiple myeloma .
Synonyms: (±)-2-Hexyl-4-pentynoic acid
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2-Hexyl-4-pentynoic acid ((±)-2-Hexyl-4-pentynoic acid), a Valproic acid (HY-10585) derivative, exhibits potential roles of HDAC inhibition (IC50 = 13 μM) and HSP70 induction. 2-Hexyl-4-pentynoic acid causes histone hyperacetylation and protect against glutamate-induced excitotoxicity in cultured neurons. 2-Hexyl-4-pentynoic acid can be used for the study of breast carcinoma. 2-Hexyl-4-pentynoic acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .
Cat. No.: HY-178773
CAS No.: 858032-59-4
SIRT2-IN-18 (Compound 8) is a SIRT2 inhibitor with IC50s of 5.3 and 12.3 μM for SmSIRT2 and hSIRT2, respectively. SIRT2-IN-18 shows potent antischistosomal activities against both Liberian and Puerto Rican strains of Schistosoma mansoni and reduces schistosomula and adult worm pair viability, pairing, and egg production, with low cytotoxicity in mammalian cells. SIRT2-IN-18 increases histone H3 hyperacetylation and induces cytochrome c-mediated apoptosis .
Cat. No.: HY-169922
HDAC-IN-82 (Compound 18b) is a histone deacetylase (HDAC) inhibitor with selective antiplasmodial and anticancer activity. HDAC-IN-82 shows potent antiproliferative activity and caspase 3/7 activation in cancer cells. HDAC-IN-82 causes hyperacetylation of histone H3 and α-tubulin .
Cat. No.: HY-121512
CAS No.: 617690-98-9
SK-7041 is a HDAC inhibitor with the IC50 of 172 nM. SK-7041 induces the hyperacetylation of histones H3 and H4 .SK-7041 inhibits tumor cell growth in vivo and in vitro, induces cell apoptosis, and arrests cell cycle at the G1 phase .
Cat. No.: HY-117136
CAS No.: 213262-83-0
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AN-7 is an orally active histone deacetylase (HDAC) inhibitor that induces histone hyperacetylation and differentiation in vitro and in vivo, and inhibits the proliferation of human prostate 22Rv1 cancer cells. AN-7 can increase the expression of the pro-apoptotic protein Bax, reduce the expression of the anti-apoptotic protein Bcl-2, and promote apoptosis by activating caspase-3, and can be used in the study of prostate cancer .
Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities .
Cat. No.: HY-156094
CAS No.: 2883046-06-6
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JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HDAC1, IC50=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion .
Cat. No.: HY-P3303
CAS No.: 146556-41-4
PF1070A is a Pf HDAC1 inhibitor with an IC50 of 0.0011 μM. By inhibiting histone deacetylase (HDAC) activity, PF1070A induces histone H4 hyperacetylation and chromatin remodeling, arrests cell cycle progression prior to nuclear division, and exhibits antimalarial activity against multidrug-resistant Plasmodium falciparum strains with high selectivity. PF1070A is suitable for use in malaria research .
Cat. No.: HY-116267
CAS No.: 1326750-61-1
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MHY219 is a histone deacetylase (HDAC) inhibitor with an IC50 of 0.276 μM. MHY219 inhibits total HDAC enzyme activity, increases histone H3 and H4 hyperacetylation. MHY219 induces cance cells phase arrest, apoptosis and inhibits proliferationin. MHY219 increases cleavage of PARP, Bax, cytochrome c levels, androgen receptor expression and decreases Bcl-2 expression. MHY219 can be used for the research of prostate cancer .
Cat. No.: HY-124792
CAS No.: 937727-03-2
MRLB-223 is a preferential HDAC1 and HDAC2 inhibitor with activity against tumor cells.MRLB-223 induces histone hyperacetylation, intrinsic apoptotic pathway activation, tumor cell apoptosis, Hsp90 hyperacetylation, and caspase-dependent Bcr-Abl degradation.MRLB-223 mediates p53-independent tumor cell death, with activity suppressed by Bcl-2 overexpression, and kills Bcr-Abl-expressing myeloid cells.MRLB-223 exerts effects in mice bearing Eμ-myc lymphomas.MRLB-223 can be used for the research of Eμ-myc lymphoma .
Cat. No.: HY-189074
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JN210 is a dual inhibitor of DCN1 and HDAC, with an IC50 of 94.26 nM against human DCN1. JN210 disrupts the UBE2M-DCN1 protein-protein interaction, blocks the neddylation modification of cullin-RING ligases, inhibits HDAC activity and induces histone hyperacetylation. JN210 impairs DNA damage repair function, induces cell apoptosis, exerts cytotoxicity and inhibits tumor growth. JN210 can be used for the research of non-small cell lung cancer .
Cat. No.: HY-187382
HDAC8-IN-17 is a histone deacetylase 8 inhibitor with human IC50 values of 0.08 μM, 0.44 μM, and 1.9 μM, and high selectivity over HDAC1, HDAC2, HDAC3, and HDAC6. HDAC8-IN-17 exhibits slow-binding, reversible uncompetitive inhibition via allosteric binding to the enzyme-substrate complex. HDAC8-IN-17 induces selective hyperacetylation of SMC3. HDAC8-IN-17 can be used for the research of cancer .
Cat. No.: HY-P12219
Synonyms: OP449
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COG449 (OP449) is a cell-penetrating peptide that binds to SET, prevents the formation of the SET-PP2A complex, and restores PP2A phosphatase activity. COG449 decreases the phosphorylation levels of AKT 308, ERK1/2, NFkB p65, and c-MYC S62, and reduces c-MYC stability and target gene expression. COG449 induces apoptosis, autophagy, and histone H3 hyperacetylation, and decreases the levels of SET, CIP2A, SETBP1, and Mcl-1. COG449 reduces cancer cell viability and decreases tumor mass in xenograft models. COG449 can be used for research on various cancers such as oral squamous cell carcinoma, T-cell acute lymphoblastic leukemia, B-CLL, non-Hodgkin lymphoma, and 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
