Search Result

Results for "

H3 acetylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (8) Bcl-2 Family (2) Caspase (4) DNA/RNA Synthesis (1) Endothelin Receptor (1) Epigenetic Reader Domain (1) Ferroptosis (2) Filovirus (2) Flavivirus (2) Fungal (1) HDAC (17) Histone Acetyltransferase (10) Histone Demethylase (1) Histone Methyltransferase (5) Keap1-Nrf2 (2) Kisspeptin Receptor (3) MDM-2/p53 (1) Microtubule/Tubulin (3) NF-κB (1) NOD-like Receptor (NLR) (2) PI3K (2) Reactive Oxygen Species (ROS) (3) Sirtuin (3) Topoisomerase (1)
By Research Areas:	Cancer (26) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (1) Metabolic Disease (2) Neurological Disease (7)

By Targets:

Apoptosis (8)

Bcl-2 Family (2)

Caspase (4)

DNA/RNA Synthesis (1)

Endothelin Receptor (1)

Epigenetic Reader Domain (1)

Ferroptosis (2)

Filovirus (2)

Flavivirus (2)

Fungal (1)

HDAC (17)

Histone Acetyltransferase (10)

Histone Demethylase (1)

Histone Methyltransferase (5)

Keap1-Nrf2 (2)

Kisspeptin Receptor (3)

MDM-2/p53 (1)

Microtubule/Tubulin (3)

NF-κB (1)

NOD-like Receptor (NLR) (2)

PI3K (2)

Reactive Oxygen Species (ROS) (3)

Sirtuin (3)

Topoisomerase (1)

By Research Areas:

Cancer (26)

Cardiovascular Disease (1)

Infection (3)

Inflammation/Immunology (1)

Metabolic Disease (2)

Neurological Disease (7)

Inhibitors & Agonists

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N4118

Cephaeline 1 Publications Verification (-)-Cephaeline; NSC 32944 free base	Filovirus Flavivirus Keap1-Nrf2 Ferroptosis Reactive Oxygen Species (ROS)	Infection Cancer
Cephaeline ((-)-Cephaeline), a desmethyl analog of Emetine, is a phenolic alkaloid in Indian Ipecac roots isolated from the Cephaelis ipecacuanha. Cephaeline exhibits potent inhibition of both Zika virus (ZIKV) and Ebola virus (EBOV) infections. Cephaeline is an inductor of histone H3 acetylation and an inhibitor of mucoepidermoid carcinoma cancer stem cells (MEC), which promotes ferroptosis by inhibiting NRF2 to exert anti-lung cancer efficacy .

HY-109109

Alteminostat CKD-581	HDAC Apoptosis	Cancer
Alteminostat (CKD-581) is a potent HDAC inhibitor. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat can be used for lymphoma and multiple myeloma research .

HY-18935

CBL0137 Maximum Cited Publications 10 Publications Verification Curaxin 137; CBL-C137	Histone Acetyltransferase MDM-2/p53 NF-κB	Cancer
CBL0137, a curaxin compound, is a histone chaperone facilitates chromatin transcription (FACT) inhibitor. CBL0137 downregulates NF-?B and activates p53. CBL0137 restores both histone H3 acetylation and trimethylation. CBL0137 is an anticancer agent. CBL0137 induces cancer cell apoptosis .

HY-W013274

CPTH2 1 Publications Verification	Histone Acetyltransferase Apoptosis	Cancer
CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B) .

HY-N4118R

Cephaeline (Standard)	Filovirus Flavivirus Keap1-Nrf2 Ferroptosis Reactive Oxygen Species (ROS)	Infection Cancer
Cephaeline ((-)-Cephaeline), a desmethyl analog of Emetine, is a phenolic alkaloid in Indian Ipecac roots isolated from the Cephaelis ipecacuanha. Cephaeline exhibits potent inhibition of both Zika virus (ZIKV) and Ebola virus (EBOV) infections. Cephaeline is an inductor of histone H3 acetylation and an inhibitor of mucoepidermoid carcinoma cancer stem cells (MEC), which promotes ferroptosis by inhibiting NRF2 to exert anti-lung cancer efficacy .

HY-117688

WJ35435	HDAC Topoisomerase Apoptosis	Cancer
WJ35435 is a dual-targeted anticancer hybrid that induces anti-HDAC (in particular HDAC1 and HDAC6) and anti-topoisomerase I activities that causes DNA damage associated with a low DNA repair capability and induces cell cycle arrest at G1- and G2-phase to apoptosis. WJ35435 induces histone H3 acetylation and phosphorylation, α-tubulin acetylation and γ-H2AX formation to achieve anti-HDAC effect. WJ35435 is promising for research of cancer .

HY-157295

PI3K/HDAC-IN-3	PI3K HDAC	Cancer
PI3K/HDAC-IN-3 (36) is a PI3K and HDAC dual inhibitor, with IC₅₀ values of 0.23 nM and 172 nM for PI3Kα and HDAC1, respectively. PI3K/HDAC-IN-3 (36) suppresses AKT phosphorylation and increased H3 acetylation in MV4-11 cells. PI3K/HDAC-IN-3 (36) exhibits significant and dose-dependent anticancer efficacy in a MV4-11 xenograft model .

HY-178333

HDAC6-IN-66	HDAC	Cancer
HDAC6-IN-66 is a potent and selective histone deacetylase (HDAC) 6 inhibitor with an IC₅₀ of 1.8 nM. HDAC6-IN-66 induces α-tubulin acetylation over histone H3. HDAC6-IN-66 can be used for the research of cancer .

HY-W013274A

CPTH2 hydrochloride	Histone Acetyltransferase Apoptosis	Cancer
CPTH2 hydrochloride is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 hydrochloride induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B) .

HY-101780A

Tinostamustine hydrochloride EDO-S101 hydrochloride; NL-101 hydrochloride	HDAC	Cancer
Tinostamustine hydrochloride (EDO-S101 hydrochloride) is a compound with anti-multiple myeloma activity and the ability to promote CD38 expression. Tinostamustine hydrochloride enhances the sensitivity of tumor cells to the anti-CD38 monoclonal antibody daratumumab by increasing the acetylation level of histone H3. Tinostamustine hydrochloride can increase the expression of MICA and MICB, thereby activating NK cells. Tinostamustine hydrochloride can significantly delay tumor growth and improve the survival rate of mice .

HY-151153

HDAC1-IN-5	HDAC Microtubule/Tubulin Caspase Apoptosis	Cancer
HDAC1-IN-5 is a potent HDAC1 inhibitor with IC₅₀ values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice .

HY-116818

Crebinostat	HDAC	Neurological Disease
Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC₅₀ values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice .

HY-178351

HDAC6-IN-67	HDAC Microtubule/Tubulin Apoptosis Caspase Bcl-2 Family	Cancer
HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer .

HY-174396

PI3Kδ/HDAC6-IN-1	PI3K HDAC Bcl-2 Family Caspase Reactive Oxygen Species (ROS) Apoptosis Histone Methyltransferase Microtubule/Tubulin	Cancer
PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC₅₀ values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3 .

HY-18700

BRD73954 4 Publications Verification	HDAC	Cancer
BRD73954 is a potent HDAC inhibitor and selectively inhibiting both HDAC6 and HDAC8 with IC₅₀ values of 0.0036, 0.12, 9, 12, 23 µM for HDAC6, HDAC8, HDAC2, HDAC1 and HDAC3, respectively. BRD73954 decreases the levels of HDAC6, associated with upregulation of Ac-Tubulin .

HY-151812

CBP/p300-IN-20	Histone Acetyltransferase Epigenetic Reader Domain	Cancer
CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC₅₀ of 10.1 for p300. CBP/p300-IN-20 can be used for the research of cancer .

HY-125969

Rtt109 inhibitor 1	Histone Acetyltransferase Fungal	Infection
Rtt109 inhibitor 1 (Compound 1) is an inhibitor for histone acetyltransferase Rtt109 through a tight binding, uncompetitive system. Rtt109 inhibitor 1 exhibits antifungal activity through acetylation at H3K56 site .

HY-W025074

BML-278	Sirtuin Histone Methyltransferase	Cancer
BML-278 is a SIRT1 activator (EC₁₅₀: 1 μM). BML-278 increases H3K9 methylation and inhibits H3K9 acetylation in both the paternal and maternal pronucleus. BML-278 improves early embryonic development. BML-278 arrests the cell cycle at the G1/S phase, and reduces senescence in primary human mesenchymal cells. BML-278 reduces tubulin acetylation in U937 cells. BML-278 also increases mitochondrial density in murine C2C12 myoblasts .

HY-123194

SIRT2/6-IN-1	Histone Demethylase Sirtuin	Metabolic Disease
SIRT2/6-IN-1 (Compound 5) is a SIRT6/SIRT2 inhibitor, with IC₅₀s of 106 μM and 114 μM. SIRT2/6-IN-1 increases H3K9 acetylation, increases glucose uptake and reduces TNF-α secretion in cells .

HY-117583A

BG47	HDAC Histone Methyltransferase	Neurological Disease
BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. BG47 can bind to and competitively inhibits the deacetylase activity of HDAC targets upon a light-induced trans-to-cis isomerization, and increases Histone Methyltransferase H3K9 acetylation. BG47 can be used for neurological disease research .

HY-117709

BRD6688	HDAC	Neurological Disease
BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model .

HY-103721

SIRT6-IN-2	Sirtuin	Metabolic Disease Inflammation/Immunology Cancer
SIRT6-IN-2 (Compound 5) is a selective and competitive SIRT6 inhibitor (IC₅₀: 34 μM). SIRT6-IN-2 increases acetylation of H3K9 and increases glucose uptake in cultured cells. SIRT6-IN-2 also reduces T cell proliferation. SIRT6-IN-2 has immunosuppressive and chemosensitizing effects .

HY-117583

cis-BG47	HDAC Histone Methyltransferase	Neurological Disease
cis-BG47 is an cis-isomer of BG47, BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. BG47 can bind to and competitively inhibits the deacetylase activity of HDAC targets upon a light-induced trans-to-cis isomerization, and increases Histone Methyltransferase H3K9 acetylation. cis-BG47 can be used for neurological disease research .

HY-146351

HDAC-IN-38	HDAC	Neurological Disease
HDAC-IN-38 (compound 13) is a potent HDAC inhibitor. HDAC-IN-38 shows similar micro-molar inhibitory activity toward HDAC1, 2, 3, 5, 6, and 8. HDAC-IN-38 increases cerebral blood flow (CBF), attenuates cognitive impairment, and improves hippocampal atrophy. HDAC-IN-38 also increases the level of histone acetylation (H3K14 or H4K5) .

HY-177044

KAT6A/KAT7-IN-2	Histone Acetyltransferase	Cancer
KAT6A/KAT7-IN-2 (Example 177) is a KAT6A and KAT7 inhibitor. KAT6A/KAT7-IN-2 has IC₅₀ values of both ≤ 1 nM for KAT6A and KAT7. KAT6A/KAT7-IN-2 can inhibit the acetylation of *H3K14* and *H3K23. KAT6A/KAT7-IN-2 also inhibits tumor cell proliferation, with an IC₅₀* of ≤ 100 nM for CAMA-1. KAT6A/KAT7-IN-2 can be used in the study of cancer .

HY-177046

KAT6A/KAT7-IN-4	Histone Acetyltransferase	Cancer
KAT6A/KAT7-IN-4 (Example 230) is a KAT6A and KAT7 inhibitor. KAT6A/KAT7-IN-4 has IC₅₀ values of both ≤ 1 nM for KAT6A and KAT7. KAT6A/KAT7-IN-4 can inhibit the acetylation of *H3K14* and *H3K23. KAT6A/KAT7-IN-4 also inhibits tumor cell proliferation, with an IC₅₀* of ≤ 100 nM for CAMA-1. KAT6A/KAT7-IN-4 can be used in the study of cancer .

HY-P1016

BQ-3020	Endothelin Receptor	Cardiovascular Disease
BQ-3020 is a selective endothelin receptor (ET_B receptor) agonist that displaces [ ¹²⁵I] ET-1 binding to ET_B receptors, with an IC₅₀ value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research ¹ ².

HY-177043

KAT6A/KAT7-IN-1	Histone Acetyltransferase	Cancer
KAT6A/KAT7-IN-1 (Example 113) is a KAT6A and KAT7 inhibitor. The IC₅₀ of KAT6A/KAT7-IN-1 for KAT6A is > 1 nM but ≤ 10 nM, while the IC₅₀ for KAT7 is ≤ 1 nM. KAT6A/KAT7-IN-1 can inhibit the acetylation of *H3K14* and *H3K23. KAT6A/KAT7-IN-1 also inhibits tumor cell proliferation, with an IC₅₀* of > 2 μM but ≤ 5 μM for CAMA-1. KAT6A/KAT7-IN-1 can be used in the study of cancer .

HY-177045

KAT6A/KAT7-IN-3	Histone Acetyltransferase	Cancer
KAT6A/KAT7-IN-3 (Example 191) is a KAT6A and KAT7 inhibitor. The IC₅₀ of KAT6A/KAT7-IN-3 for KAT6A is ≤ 50 nM and > 10 nM, while the IC₅₀ for KAT7 is ≤ 1 nM. KAT6A/KAT7-IN-3 can inhibit the acetylation of *H3K14* and *H3K23. KAT6A/KAT7-IN-3 also inhibits tumor cell proliferation, with an IC₅₀* of > 2 μM and ≤ 5 μM for CAMA-1. KAT6A/KAT7-IN-3 can be used in the study of cancer .

HY-156096

HDAC3-IN-2	HDAC Histone Methyltransferase Caspase Apoptosis DNA/RNA Synthesis	Cancer
HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC₅₀: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC₅₀ of 0.55 μM against 4T1 and an IC₅₀ of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .

HY-176244

KI-TOX-A3	Histone Acetyltransferase	Cancer
KI-TOX-A3 is a selective protein-protein interaction (PPI) inhibitor targeting TOX protein (with an IC₅₀ value of 0.51 μM for TOX-KAT7 interaction). KI-TOX-A3 induces proteasomal degradation of TOX, restores KAT7-mediated H3K14 acetylation, reversing CD8 ⁺ T cell exhaustion and inhibiting T-cell acute lymphoblastic leukemia (T-ALL) cell proliferation. KI-TOX-A3 is promising for research of hematological tumors (e.g., T-ALL) .

HY-176867

Rodin-B	HDAC	Neurological Disease
Rodin-B is a selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC₅₀ value of 0.50 μM for the CoREST complex, 0.27 μM for HDAC1, and 0.28 μM for HDAC2. Rodin-B increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-B is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease .

HY-176866

Rodin-A	HDAC	Neurological Disease
Rodin-A is an orally active, brain-penetrant and selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC₅₀ value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. Rodin-A increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-A is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease .

HY-P5544

M-TriDAP N-Acetylmuramyl-L-Ala-γ-D-Glu-meso-diaminopimelic acid	NOD-like Receptor (NLR)	Others
M-TriDAP (N-Acetylmuramyl-L-Ala-γ-D-Glu-meso-diaminopimelic acid) is a NOD1/2 agoist and biological active peptide .

HY-P5544A

M-TriDAP TFA N-Acetylmuramyl-L-Ala-γ-D-Glu-meso-diaminopimelic acid TFA	NOD-like Receptor (NLR)	Others
M-TriDAP (N-Acetylmuramyl-L-Ala-γ-D-Glu-meso-diaminopimelic acid) TFA is a NOD1/2 agoist and biological active peptide .

HY-P2161B

TAK-683 acetate 1 Publications Verification	Kisspeptin Receptor	Cancer
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC₅₀ values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .

HY-P2161A

TAK-683 TFA	Kisspeptin Receptor	Cancer
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC₅₀ values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .

HY-P2161

TAK-683	Kisspeptin Receptor	Cancer
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC₅₀ values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .

Cat. No.	Product Name	Target	Research Area