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Results for "

phosphorylation inhibitory activity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (2) AMPK (1) Apoptosis (6) Btk (1) c-Fms (1) c-Kit (1) Casein Kinase (1) Caspase (1) CDK (1) Checkpoint Kinase (Chk) (1) ERK (2) FGFR (1) GSK-3 (1) HDAC (2) Interleukin Related (7) JAK (4) MARCKS (1) MEK (1) NF-κB (2) PARP (1) PDGFR (1) PKC (1) Raf (2) Ras (2) Reference Standards (1) Ribosomal S6 Kinase (RSK) (1) Src (1) STAT (5) STING (1) TAM Receptor (1) Tau Protein (1) TGF-β Receptor (1) Tie (1) TNF Receptor (3) Tyrosinase (3) VEGFR (2)
By Research Areas:	Cancer (13) Endocrinology (1) Inflammation/Immunology (13) Neurological Disease (1)

By Targets:

Akt (2)

AMPK (1)

Apoptosis (6)

Btk (1)

c-Fms (1)

c-Kit (1)

Casein Kinase (1)

Caspase (1)

CDK (1)

Checkpoint Kinase (Chk) (1)

ERK (2)

FGFR (1)

GSK-3 (1)

HDAC (2)

Interleukin Related (7)

JAK (4)

MARCKS (1)

MEK (1)

NF-κB (2)

PARP (1)

PDGFR (1)

PKC (1)

Raf (2)

Ras (2)

Reference Standards (1)

Ribosomal S6 Kinase (RSK) (1)

Src (1)

STAT (5)

STING (1)

TAM Receptor (1)

Tau Protein (1)

TGF-β Receptor (1)

Tie (1)

TNF Receptor (3)

Tyrosinase (3)

VEGFR (2)

By Research Areas:

Cancer (13)

Endocrinology (1)

Inflammation/Immunology (13)

Neurological Disease (1)

Inhibitors & Agonists

Peptides

Natural
Products

Targets Recommended: Oxidative Phosphorylation Macrophage migration inhibitory factor (MIF) DYRK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-122198

ML367	Checkpoint Kinase (Chk)	Cancer
ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation .

HY-N10472

STAT3-IN-14	STAT	Cancer
STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3 .

HY-112693

H-151 Maximum Cited Publications 89 Publications Verification	STING	Inflammation/Immunology
H-151 is a potent, selective and covalent antagonist of STING that has noteworthy inhibitory activity both in cells and in vivo. H-151 reduces TBK1 phosphorylation and suppresses STING palmitoylation. H-151 can be used for the research of autoinflammatory disease .

HY-155805

CAF-382	CDK	Cancer
CAF-382 (compound B1) is an analog of SNS-032 and a CDKL5 and pan-CDK inhibitor with a weak GSK3α/β affinity (>1.8 μM) and inhibitory activity. CAF-382 inhibits CDKL5 and blocks the phosphorylation of the CDKL5 E2 domain .

HY-143884

JAK2/TYK2-IN-1	JAK	Inflammation/Immunology
JAK2/TYK2-IN-2 is a potent and selective TYK2 inhibitor with IC₅₀ values of 9 and 157 nM for TYK2 and JAK2, respectively. JAK2/TYK2-IN-2 has anti-inflammatory activity .

HY-N8646

Isodonal	Others	Cancer
Isodonal is a N-pentane diterpene compound with potential cytotoxic, antitumor, inhibitory oxidative phosphorylation and antiingestion activities. Isodonal can be isolated from the leaves of Isodon wikstroemioides and is used in the study of gastrointestinal diseases, anti-tumor and anti-inflammatory .

HY-143900

BTK-IN-7	Btk Apoptosis	Inflammation/Immunology Cancer
BTK-IN-7 is a potent and selective inhibitor of BTK (IC₅₀=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels (ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity .

HY-168079

GSK-3β inhibitor 21	GSK-3 Tau Protein	Neurological Disease Inflammation/Immunology
GSK-3β inhibitor 21 (compound 44) is an ATP-competitive GSK-3β inhibitor (IC₅₀=6.06 μM) with anti-amyloid aggregation and tau phosphorylation inhibitory activities. GSK-3β inhibitor 21 can be used in the study of Alzheimer's disease .

HY-118668

ABD-350	NF-κB	Others
ABD-350 is an antiresorptive agent that inhibits osteoclast activity without affecting osteoblast activity and preventing ovariectomy-induced bone loss. ABD-350 inhibits NF-κB ligand-induced inhibitor of NF-κB phosphorylation, leading to osteoclast apoptosis, but has no inhibitory effect on osteoblast function, effectively preventing bone loss in ovariectomized mice, and does not inhibit parathyroid hormone-induced bone formation.

HY-157298

anti-TNBC agent-4	Apoptosis	Cancer
anti-TNBC agent-4 (compound 7) exhibits highly inhibitory activity against different TNBC cells with IC₅₀s from 0.37 μM to 1.52 μM. anti-TNBC agent-4 inhibits IKKβ mediated phosphorylation of IκB and p65. anti-TNBC agent-4 induces TNBC cells apoptosis .

HY-N0619

Mulberroside A 3 Publications Verification	TNF Receptor Interleukin Related Tyrosinase	Inflammation/Immunology
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC₅₀ of 53.6 μM .

HY-118528A

TP0427736 hydrochloride 1 Publications Verification	TGF-β Receptor	Endocrinology
TP0427736 hydrochloride is a potent inhibitor of ALK5 kinase activity with an IC₅₀ of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC₅₀=836 nM). TP0427736 hydrochloride also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC₅₀ value of 8.68 nM. TP0427736 hydrochloride can be used for the research of androgenic alopecia (AGA) .

HY-150026

Multi-kinase-IN-2	VEGFR PDGFR FGFR c-Kit Akt Src Apoptosis	Cancer
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity .

HY-N0619A

cis-Mulberroside A Mulberroside D	TNF Receptor Interleukin Related Tyrosinase	Inflammation/Immunology
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC₅₀ of 53.6 μM .

HY-173400

UNC8212	TAM Receptor	Cancer
UNC8212 is a TAM kinase inhibitor. UNC8212 has potent inhibitory activity against MERTK and AXL (IC₅₀: 1.5 nM and 1.3 nM, respectively), and also inhibits TYRO3 (IC₅₀: 6.7 nM). UNC8212 mediates polypharmacological properties by targeting the structurally diverse "back pocket" region of the TAM kinase family. UNC8212 binds tightly to TAM kinases and potently inhibits MERTK and AXL phosphorylation. UNC8212 has anti-tumor effects and can be used in cancer immunotherapy and tumor cell targeting research .

HY-N0619R

Mulberroside A (Standard)	Reference Standards TNF Receptor Interleukin Related Tyrosinase	Inflammation/Immunology
Mulberroside A (Standard) is the analytical standard of Mulberroside A. This product is intended for research and analytical applications. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC₅₀ of 53.6 μM .

HY-171038

STAT3-IN-39	STAT	Inflammation/Immunology
STAT3-IN-39 (compound 10K) is an orally active STAT3 inhibitor that exhibits excellent inhibitory activity against STAT3 phosphorylation, with an IC₅₀ of 0.47 μM in NIH-3T3 cells. STAT3-IN-39 inhibits the TGF-β1-induced fibrotic response and blocks the epithelial-mesenchymal transition in A549. STAT3-IN-39 can be utilized in research related to idiopathic pulmonary fibrosis .

HY-156498

RMC-7977 5+ Cited Publications	Ras ERK Raf Ribosomal S6 Kinase (RSK) AMPK Apoptosis PARP	Cancer
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (K_d = 195 nM) and KRAS (G12V) (K_d = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS ^G12C cancer models, and demonstrates good tolerability across various RAS cancer models .

HY-124295

Imofinostat ABT-301; MPT0E028; TMU-C-0012	HDAC Akt Apoptosis	Inflammation/Immunology Cancer
Imofinostat (ABT-301; MPT0E028) is an orally active and selective HDAC inhibitor with IC₅₀s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. Imofinostat has a weak inhibitory effect on HDAC8 (IC₅₀ of 2.5 μM), but no inhibitory effect on HDAC4 (IC₅₀>10 μM). Imofinostat reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. Imofinostat has a broad-spectrum antitumor activity, including colorectal cancer, B-cell lymphoma, non-small cell lung carcinoma (NSCLC), and pancreatic cancer, while also showing therapeutic potential in non-tumor diseases like emphysema and pulmonary fibrosis .

HY-176561

IOR-160	Casein Kinase HDAC	Cancer
IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC₅₀ = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC₅₀s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research .

HY-100754C

Ritlecitinib tosylate 5+ Cited Publications PF-06651600 tosylate	JAK Interleukin Related STAT	Inflammation/Immunology
Ritlecitinib (PF-06651600) tosylate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib tosylate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib tosylate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .

HY-100754

Ritlecitinib 5+ Cited Publications PF-06651600	JAK Interleukin Related STAT	Inflammation/Immunology
Ritlecitinib (PF-06651600) is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .

HY-100754A

Ritlecitinib (malonate) PF-06651600 (malonate)	JAK Interleukin Related STAT	Inflammation/Immunology
Ritlecitinib (PF-06651600) malonate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib malonate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib malonate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .

HY-164529

SJ-C1044	Raf Ras MEK ERK VEGFR Tie c-Fms	Cancer
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC₅₀ values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC₅₀ values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .

HY-P5439

Epsilon-V1-2, Cys-conjugated	PKC MARCKS	Others
Epsilon-V1-2, Cys-conjugated is a biological active peptide. (This peptide is the εPKC specific inhibitor. Its inhibitory activity is based on εPKC translocation and MARCKS phosphorylation. This peptide interferes with εPKC interaction with the anchoring protein εRACK. This peptide contains a cysteine residue added to the C-terminus for potential S-S bond formation with a carrier protein.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)

HY-155759

HMGB1-IN-2	NF-κB Interleukin Related Caspase Apoptosis	Inflammation/Immunology Cancer
HMGB1-IN-2 (compound 15) is an inhibitor of highly conserved nuclear protein (HMGB1), showing NO inhibitory effect with IC₅₀ value of 20.2 μM in RAW264.7 cells. HMGB1-IN-2 (30 μM) decreases the level of IL-1 β, TNF-α, caspase-1 p20, inhibits the phosphorylation of NF-κB p65, exhibits anti-apoptotic activity. HMGB1-IN-2 (15 mg/kg; ip) relives kidney injury in septic acute kidney injury mouse. HMGB1-IN-2 inhibits Huh7 cells and A549 cells with IC₅₀s of 77.0 μM, and 82.0 μM, respectively .

Cat. No.	Product Name	Target	Research Area

HY-P5439

Epsilon-V1-2, Cys-conjugated	PKC MARCKS	Others
Epsilon-V1-2, Cys-conjugated is a biological active peptide. (This peptide is the εPKC specific inhibitor. Its inhibitory activity is based on εPKC translocation and MARCKS phosphorylation. This peptide interferes with εPKC interaction with the anchoring protein εRACK. This peptide contains a cysteine residue added to the C-terminus for potential S-S bond formation with a carrier protein.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)

STAT3-IN-14	Nicotiana tabacum L. Source classification Plants Solanaceae Naphthalene Quinones	STAT
STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3 .

Mulberroside A 3 Publications Verification	Structural Classification Stilbenes Classification of Application Fields Source classification Phenols Polyphenols Morus alba L. Plants Moraceae Inflammation/Immunology Disease Research Fields	TNF Receptor Interleukin Related Tyrosinase
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC₅₀ of 53.6 μM .

Isodonal	Structural Classification Terpenoids Labiatae Source classification Cirsium palustre (L.) Scop. Diterpenoids Plants	Others
Isodonal is a N-pentane diterpene compound with potential cytotoxic, antitumor, inhibitory oxidative phosphorylation and antiingestion activities. Isodonal can be isolated from the leaves of Isodon wikstroemioides and is used in the study of gastrointestinal diseases, anti-tumor and anti-inflammatory .

cis-Mulberroside A Mulberroside D	Stilbenes Classification of Application Fields Source classification Phenols Polyphenols Plants Moraceae Inflammation/Immunology Disease Research Fields Morus alba Linn.	TNF Receptor Interleukin Related Tyrosinase
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC₅₀ of 53.6 μM .

Mulberroside A (Standard)	Structural Classification Stilbenes Source classification Phenols Polyphenols Morus alba L. Plants Moraceae	Reference Standards TNF Receptor Interleukin Related Tyrosinase
Mulberroside A (Standard) is the analytical standard of Mulberroside A. This product is intended for research and analytical applications. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC₅₀ of 53.6 μM .

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