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Results for "

Histone phosphorylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	HDAC (5) Histone Methyltransferase (1) Akt (2) AMPK (1) Apoptosis (9) ATM/ATR (1) Aurora Kinase (5) Autophagy (1) Bcr-Abl (1) c-Myc (1) Checkpoint Kinase (Chk) (1) CMV (2) EBV (2) Endogenous Metabolite (1) FLAP (1) Haspin Kinase (2) Isotope-Labeled Compounds (1) JAK (1) mTOR (1) p38 MAPK (1) PDGFR (2) PI3K (3) PKA (1) PKC (2) Polo-like Kinase (PLK) (3) Reference Standards (1) Topoisomerase (1) VEGFR (2)
By Research Areas:	Cancer (18) Infection (2) Metabolic Disease (1)

By Targets:

HDAC (5)

Histone Methyltransferase (1)

Akt (2)

AMPK (1)

Apoptosis (9)

ATM/ATR (1)

Aurora Kinase (5)

Autophagy (1)

Bcr-Abl (1)

c-Myc (1)

Checkpoint Kinase (Chk) (1)

CMV (2)

EBV (2)

Endogenous Metabolite (1)

FLAP (1)

Haspin Kinase (2)

Isotope-Labeled Compounds (1)

JAK (1)

mTOR (1)

p38 MAPK (1)

PDGFR (2)

PI3K (3)

PKA (1)

PKC (2)

Polo-like Kinase (PLK) (3)

Reference Standards (1)

Topoisomerase (1)

VEGFR (2)

By Research Areas:

Cancer (18)

Infection (2)

Metabolic Disease (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Isotope-Labeled Compounds

Targets Recommended: Oxidative Phosphorylation Histone Methyltransferase Histone Demethylase Histone Acetyltransferase HDAC DYRK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P5988

N-myristoyl-RKRTLRRL	PKC	Cancer
N-myristoyl-RKRTLRRL inhibits binding of PKC substrates. N-myristoyl-RKRTLRRL inhibits Ca ²⁺- and phosphatidylserine (PS)-dependent histone phosphorylation with IC₅₀ of 5 μM. histone phosphorylation with IC₅₀ of 80 μM .

HY-16305

Maribavir Maximum Cited Publications 12 Publications Verification 1263W94; BW1263W94; GW257406X	EBV CMV	Infection
Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC₅₀ of 3 nM. Maribavir has potent antiviral activity against HCMV and Epstein-Barr virus (EBV).

HY-15217

CHR-6494 5+ Cited Publications	Haspin Kinase	Cancer
CHR-6494 is a potent inhibitor of haspin, with an IC₅₀ of 2 nM. CHR-6494 inhibits histone H3T3 phosphorylation. CHR-6494 can be used in the research of cancer .

HY-16305S

Maribavir-d6 1263W94-d₆; BW1263W94-d₆; GW257406X-d₆	Isotope-Labeled Compounds	Others
Maribavir-d₆ (1263W94-d₆) is a deuterium labeled Maribavir (HY-16305). Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC₅₀ of 3 nM .

HY-P3745

*H1-7 (histone* H1 phosphorylation site), PKA Substrate**	PKA	Others
H1-7 (histone H1 phosphorylation site), PKA Substrate, a synthetic polypeptide, can be used as PKA substrate .

HY-P1371

Pseudo RACK1 KKWKMRRNQFWIKIQRC CSVEIWD*	PKC	Others
Pseudo RACK1, a peptide, is a PKC agonist with homologous sequences of PKC. Pseudo RACK1 interacts selectively with β-PKC at an autoregulatory site (RACK-binding site) and activates it in the absence of PKC activators, following inducing PKC-mediated histone phosphorylation .

HY-149283

JAK/HDAC-IN-2	JAK HDAC Apoptosis	Cancer
JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers .

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-P1115

AKTide-2T	Akt	Others
AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a K_i of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .

HY-P1115A

AKTide-2T TFA	Akt	Others
AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a K_i of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .

HY-16305R

Maribavir (Standard) 1263W94 (Standard); BW1263W94 (Standard); GW257406X (Standard)	EBV Reference Standards CMV	Infection
Maribavir (Standard) is the analytical standard of Maribavir. This product is intended for research and analytical applications. Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC₅₀ of 3 nM. Maribavir has potent antiviral activity against HCMV and Epstein-Barr virus (EBV).

HY-W339757

Dioctanoylphosphatidic acid sodium	mTOR Endogenous Metabolite	Cancer
Dioctanoylphosphatidic acid sodium functions as a modulator of phagocyte respiratory burst, acts as a precursor to diacylglycerol and lysophosphatidic acid, and influences the phosphorylation of the mammalian target of rapamycin (mTOR) while enhancing the viability of gallbladder carcinoma cells treated with histone deacetylase inhibitors (HDACIs); it is derived from glycerophospholipid through the action of phospholipase D.

HY-110350

CHR-6494 TFA	Haspin Kinase	Cancer
CHR-6494 TFA is a potent inhibitor of haspin, with an IC₅₀ of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer .

HY-125158

HOI-07	Aurora Kinase Apoptosis	Cancer
HOI-07 is a selective Aurora B kinase inhibitor. HOI-07 blocks phosphorylation of histone H3 on Ser10 in lung cancer cells. HOI-07 induces cell-cycle arrest, and apoptosis. HOI-07 has antitumor activity, and suppresses the tumor growth of A549, 143B and KHOS xenografts .

HY-12037A

Rigosertib 5+ Cited Publications ON-01910	Polo-like Kinase (PLK) PI3K Apoptosis	Cancer
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC₅₀ of 9 nM .

HY-162616

SelSA	HDAC Apoptosis	Cancer
SelSA is a selective, orally active inhibitor for histone deacetylase 6 (HDAC6) with IC₅₀ of 56.9 nM. SelSA inhibits the phosphorylation of ERK1/2. SelSA inhibits the proliferation of breast cancer cells and hepatocellular carcinoma cells with IC₅₀ of 0.58-2.6 μM, inhibits cell migration and invasion of Huh7, and induces apoptosis. SelSA exhibits antitumor activity in mouse model .

HY-118034

MTBT 1 Publications Verification	p38 MAPK Apoptosis	Cancer
MTBT is an anticancer agent and p38 MAPK activator. MTBT can inhibit tumor cell proliferation, induce cell cycle arrest and apoptosis. MTBT increases the phosphorylation of histone H3 serine in cancer cells, thereby arresting the cell cycle in the M phase. The specific inhibitor of p38 MAPK, Adezmapimod (HY-10256), can abrogate the cell cycle arrest induced by MTBT .

HY-12037

Rigosertib sodium 5+ Cited Publications ON-01910 sodium	Polo-like Kinase (PLK) PI3K Apoptosis	Cancer
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC₅₀ of 9 nM .

HY-126249

AAPK-25	Aurora Kinase Polo-like Kinase (PLK) Apoptosis	Cancer
AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3 ^Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with K_d values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with K_d values ranging from 55-456 nM .

HY-125090

PHA-680626	Aurora Kinase c-Myc Bcr-Abl Histone Methyltransferase Apoptosis	Cancer
PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells .

HY-123834

FEN1-IN-1 5+ Cited Publications	FLAP ATM/ATR	Cancer
FEN1-IN-1 (compound 1) is a small molecule flap endonuclease 1 (FEN1) inhibitor with antitumor activity. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg ²⁺ ions. FEN1-IN-1 initiaties a DNA damage response and activates the ATM checkpoint signalling pathway, the phosphorylation of histone H2AX and the ubiquitination of FANCD2 in mammalian cells. FEN1-IN-1 is promising for research of cancers .

HY-16018A

Ilorasertib hydrochloride ABT-348 hydrochloride	Aurora Kinase PDGFR VEGFR	Cancer
Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC₅₀s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .

HY-16018

Ilorasertib ABT-348	Aurora Kinase VEGFR PDGFR	Cancer
Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC₅₀s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .

HY-123597

NSC 109555 DDUG; NCI C04808	Autophagy Checkpoint Kinase (Chk)	Cancer
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.

HY-172157

HDAC11-IN-2	HDAC AMPK	Metabolic Disease
HDAC11-IN-2 (compound B6) is a high selective Histone Deacetylase 11 (HDAC11) inhibitor. HDAC11-IN-2 inhibits HDAC11 and HDAC8 with IC₅₀s of 51.1 ×10 ^-3 μM and 5 μM, respectively. HDAC11-IN-2 inhibits denovolipogenesis (DNL) and promotes fatty acid oxidation, thus mitigating hepaticlipid accumulation and pathological symptoms in MASLD mice. HDAC11-IN-2 enhances the phosphorylation of AMPKα1 at Thr172 through the inhibition of HDAC11, consequently modulating DNL and fatty acid oxidation in the liver .

HY-156091

PI3Kα/HDAC6-IN-1	PI3K HDAC	Cancer
PI3Kα/HDAC6-IN-1 (compound 21j) is a dual PI3Kα/HDAC6 inhibitor with IC₅₀ of 2.9 and 26 nM, respectively. PI3Kα/HDAC6-IN-1 also inhibits AKT(Ser473) phosphorylation and induces the accumulation of acetylated α-tubulin without affecting acetylated histones H3 and H4. PI3Kα/HDAC6-IN-1 efficiently inhibits L-363 cell line (IC₅₀=0.17 μM) and has good anti-cancer activity .

Cat. No.	Product Name

HY-L024

Histone Modification Research Compound Library	807 compounds
A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases. MCE owns a unique collection of 807 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

Histone Modification Research Compound Library

807 compounds

A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases.

MCE owns a unique collection of 807 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

Cat. No.	Product Name	Target	Research Area