Search Result

Results for "

phosphorylation inhibitory activity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	DYRK (1) Macrophage migration inhibitory factor (MIF) (1) Acetyl-CoA Carboxylase (1) Akt (5) AMPK (3) Amyloid-β (2) Anaplastic lymphoma kinase (ALK) (2) Androgen Receptor (1) Angiotensin-converting Enzyme (ACE) (1) Apoptosis (14) ATP Synthase (1) Bacterial (1) Btk (1) c-Fms (1) c-Kit (1) Cannabinoid Receptor (1) Casein Kinase (1) Caspase (3) CDK (3) Checkpoint Kinase (Chk) (1) Cholinesterase (ChE) (3) COX (1) Cuproptosis (1) DNA/RNA Synthesis (1) EGFR (1) Epigenetic Reader Domain (1) ERK (7) Eukaryotic Initiation Factor (eIF) (1) Ferroptosis (1) FGFR (2) Glutathione Peroxidase (1) GSK-3 (2) HDAC (2) IKK (2) Influenza Virus (1) Interleukin Related (12) JAK (7) JNK (3) Keap1-Nrf2 (2) Large Tumor Suppressor (LATS) (2) LDLR (1) MARCKS (1) MEK (1) Mitochondrial Metabolism (1) MMP (1) Molecular Glues (1) Monoamine Oxidase (1) Mps1 (1) NF-κB (5) NO Synthase (1) p38 MAPK (5) PAK (1) PARP (1) PCSK9 (1) PDGFR (1) PERK (2) PGE synthase (1) Phosphatase (1) PI3K (1) PKA (2) PKC (1) Potassium Channel (2) PPAR (1) PROTACs (1) Raf (2) Ras (2) Reactive Oxygen Species (ROS) (4) Reference Standards (3) Ribosomal S6 Kinase (RSK) (1) SARS-CoV (1) SHP2 (1) Src (1) STAT (9) STING (1) TAM Receptor (1) Tau Protein (3) TGF-beta/Smad (1) TGF-β Receptor (1) Tie (1) TNF Receptor (5) Tyrosinase (5) VEGFR (2) Wnt (1) YAP (2) α-synuclein (1) β-catenin (2)
By Research Areas:	Cancer (31) Cardiovascular Disease (1) Endocrinology (1) Infection (3) Inflammation/Immunology (21) Metabolic Disease (4) Neurological Disease (7)

By Targets:

DYRK (1)

Macrophage migration inhibitory factor (MIF) (1)

Acetyl-CoA Carboxylase (1)

Akt (5)

AMPK (3)

Amyloid-β (2)

Anaplastic lymphoma kinase (ALK) (2)

Androgen Receptor (1)

Angiotensin-converting Enzyme (ACE) (1)

Apoptosis (14)

ATP Synthase (1)

Bacterial (1)

Btk (1)

c-Fms (1)

c-Kit (1)

Cannabinoid Receptor (1)

Casein Kinase (1)

Caspase (3)

CDK (3)

Checkpoint Kinase (Chk) (1)

Cholinesterase (ChE) (3)

COX (1)

Cuproptosis (1)

DNA/RNA Synthesis (1)

EGFR (1)

Epigenetic Reader Domain (1)

ERK (7)

Eukaryotic Initiation Factor (eIF) (1)

Ferroptosis (1)

FGFR (2)

Glutathione Peroxidase (1)

GSK-3 (2)

HDAC (2)

IKK (2)

Influenza Virus (1)

Interleukin Related (12)

JAK (7)

JNK (3)

Keap1-Nrf2 (2)

Large Tumor Suppressor (LATS) (2)

LDLR (1)

MARCKS (1)

MEK (1)

Mitochondrial Metabolism (1)

MMP (1)

Molecular Glues (1)

Monoamine Oxidase (1)

Mps1 (1)

NF-κB (5)

NO Synthase (1)

p38 MAPK (5)

PAK (1)

PARP (1)

PCSK9 (1)

PDGFR (1)

PERK (2)

PGE synthase (1)

Phosphatase (1)

PI3K (1)

PKA (2)

PKC (1)

Potassium Channel (2)

PPAR (1)

PROTACs (1)

Raf (2)

Ras (2)

Reactive Oxygen Species (ROS) (4)

Reference Standards (3)

Ribosomal S6 Kinase (RSK) (1)

SARS-CoV (1)

SHP2 (1)

Src (1)

STAT (9)

STING (1)

TAM Receptor (1)

Tau Protein (3)

TGF-beta/Smad (1)

TGF-β Receptor (1)

Tie (1)

TNF Receptor (5)

Tyrosinase (5)

VEGFR (2)

Wnt (1)

YAP (2)

α-synuclein (1)

β-catenin (2)

By Research Areas:

Cancer (31)

Cardiovascular Disease (1)

Endocrinology (1)

Infection (3)

Inflammation/Immunology (21)

Metabolic Disease (4)

Neurological Disease (7)

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-112693

H-151 Maximum Cited Publications 138 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-156498

RMC-7977 10+ 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-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-N0619

Mulberroside A 4 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-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-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-175238

KI-DX-014	ATP Synthase DNA/RNA Synthesis	Neurological Disease Cancer
KI-DX-014 is a DDX21 inhibitor with high RNA-binding inhibitory activity (IC₅₀ of 3.31 μM). KI-DX-014 targets DDX21’s intrinsically disordered C-terminal domain, inhibits DDX21-structured RNA interaction, modulates DDX21’s RNA-dependent ATPase activity, and disrupts DDX21 biomolecular condensate formation. KI-DX-014 attenuates in vitro P-TEFb release from the 7SK snRNP complex, suppresses P-TEFb-dependent RNA polymerase II CTD phosphorylation, and induces developmental defects in zebrafish embryos. KI-DX-014 acts as a chemical probe for dissecting DDX21 functions in normal physiology and disease states. KI-DX-014 can be used for cancers and neurodegenerative disorders research .

HY-122198

ML367 1 Publications Verification	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-147831

HR-19011	Eukaryotic Initiation Factor (eIF) Epigenetic Reader Domain	Cancer
HR-19011 is an eIF2α phosphorylation activator targeting heme-regulated inhibitor HRI (EIF2AK1). HR-19011 exhibits growth inhibitory activity against K562 cells with an IC₅₀ value of 3.91 µM. HR-19011 inhibits the growth of hematologic malignancies by targeting HRI to activate the integrated stress response via the HRI-eIF2α-ATF4 axis. HR-19011 shows good safety in vivo. HR-19011 can be used for research on hematologic malignancies (leukemia) .

HY-103322

6-Bnz-cAMP sodium salt	PKA Potassium Channel	Metabolic Disease Cancer
6-Bnz-cAMP sodium, a derivative of cyclic adenosine monophosphate (cAMP), is a selective PKA activator with inhibitory activity against the bTREK-1 K ⁺ channel. 6-Bnz-cAMP sodium does not activate the Epac signaling pathway. It inhibits the bTREK-1 K ⁺ channel via a voltage-independent, ATP-dependent mechanism that is independent of the PKA/Epac/calmodulin kinase/MAP kinase pathway. 6-Bnz-cAMP sodium activates CREB phosphorylation to regulate osteoblast-specific gene expression, induces osteoblast differentiation, promotes extracellular matrix mineralization, supports osteoblast proliferation, and shows no cytotoxicity toward osteoblasts. It can be used in studies related to bone tissue repair and regeneration .

HY-N3266

Methyl rosmarinate	Tyrosinase Phosphatase Cholinesterase (ChE) SARS-CoV PERK JNK p38 MAPK TGF-beta/Smad Apoptosis Reactive Oxygen Species (ROS) AMPK MMP	Cardiovascular Disease Infection Neurological Disease Inflammation/Immunology Cancer
Methyl rosmarinate is an orally active hydroxycinnamic acid. Methyl rosmarinate exhibits an IC₅₀ of 24.70 μM and a K_i of 15.29 μM against PTP1B, an IC₅₀ of 41.46 μg/mL against BChE, a K_i of 0.61 mM against mushroom tyrosinase, and an IC₅₀ of 2.50 μM against SARS-CoV-2 3CLpro. Methyl rosmarinate downregulates the phosphorylation levels of ERK, JNK, p38, Smad2 and Smad3. Methyl rosmarinate activates erythrocyte BPGM and promotes the production of 2,3-BPG. Methyl rosmarinate induces apoptosis of fibroblasts. Methyl rosmarinate prolongs the survival time of hypoxic mice. Methyl rosmarinate improves insulin sensitivity. Methyl rosmarinate binds to SARS-CoV-2 3CLpro and inhibits viral replication. Methyl rosmarinate induces glioblastoma cell death. Methyl rosmarinate activates the TGR5/AMPK axis and reduces the levels of ROS and MDA. Methyl rosmarinate shows inhibitory activity against MMP-1. Methyl rosmarinate can be used in research related to pulmonary fibrosis, hypoxia-induced injury, type 2 diabetes, Alzheimer's disease, hyperpigmentation disorders, COVID-19, glioblastoma and myocardial ischemia-reperfusion injury .

HY-171705

KMS99220	Keap1-Nrf2 AMPK JNK IKK p38 MAPK NO Synthase α-synuclein Interleukin Related	Neurological Disease
KMS99220 is an orally active, blood-brain barrier-permeable activator of the Nrf2 inhibitory protein Keap-1. KMS99220 enhances the activity of AMPK, activates the Nrf2 signaling pathway, and reduces the phosphorylation of IκB, nuclear translocation of NFκB, as well as the phosphorylation levels of JNK, IKK and p38 MAPK via HO-1. KMS99220 binds to Keap1 to trigger the nuclear translocation of Nrf2, induces the expression of HO-1, NQO1, GCLC, GCLM and proteasome subunits; enhances proteasomal enzymatic activity; inhibits iNOS expression, nitric oxide production and IL-1β generation; attenuates microglial activation; reduces α-synuclein aggregation; and prevents dopaminergic neuron degeneration and motor dysfunction. KMS99220 prevents the degeneration of dopaminergic neurons in the substantia nigra, induces the expression of Nrf2 downstream target genes, and effectively ameliorates associated motor dysfunction in a mouse model of Parkinson's disease. KMS99220 is applicable to research related to Parkinson's disease .

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-155805

SGC-CAF382-1	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-176886

LATS-IN-2	Large Tumor Suppressor (LATS) YAP	Others
LATS-IN-2 is an efficiently acting LATS (large tumor suppressor kinase) inhibitor. LATS-IN-2 shows potent inhibitory activity against LATS1 with an IC₅₀ value of 1.3 nM. LATS-IN-2 suppresses the phosphorylation of YAP by inhibiting LATS kinase activity. LATS-IN-2 increases the thickness of the epidermis in mice. LATS-IN-2 can be used for the study of ocular diseases such as limbal stem cell deficiency and corneal endothelial dysfunction .

HY-N11011

Withaphysalin A	NF-κB STAT PERK JNK p38 MAPK PGE synthase Interleukin Related TNF Receptor COX	Inflammation/Immunology Cancer
Withaphysalin A is a withanolide compound with anti-inflammatory and antioxidant activities. Withaphysalin A inhibits LPS (HY-D1056)-induced nuclear translocation of NF-κB p65, as well as phosphorylation of STAT3, ERK, JNK and p38 MAPK. Withaphysalin A upregulates the expression of HO-1. Withaphysalin A inhibits LPS-induced production of NO, PGE₂, IL-1β, IL-6 and TNF-α. Withaphysalin A downregulates LPS-induced expression of iNOS and COX-2. Withaphysalin A interacts with B-cell activating factor protein (BAFF) to exert inhibitory effects. Withaphysalin A exhibits ELOVL6 inhibitory activity. Withaphysalin A can be used in the research of inflammatory diseases, nephrotic syndrome and chronic myeloid leukemia .

HY-N1098

Velutin	Tyrosinase p38 MAPK NF-κB Bacterial	Infection Metabolic Disease Inflammation/Immunology
Velutin is a flavonoid. Velutin can be extracted from mistletoe. Velutin inhibits mushroom Tyrosinase activity with an IC₅₀ of 910.1 μM. Velutin inhibits p38 phosphorylation, the NF-κB pathway and the MAPK pathway. Velutin prevents articular cartilage degeneration and subchondral bone loss. Velutin slows down the progression of intervertebral disc degeneration. Velutin exhibits inhibitory effects on melanogenesis, skin whitening, anti-inflammatory, anti-allergic, anti-oxidant and antibacterial activities. Velutin can be used in studies related to pigmented diseases, osteoarthritis and intervertebral disc degeneration .

HY-142026

Vitisin A (+)-Vitisin A	Caspase ERK NF-κB Influenza Virus PAK LDLR PPAR PCSK9 Androgen Receptor Keap1-Nrf2 Monoamine Oxidase Cholinesterase (ChE) IKK Wnt β-catenin Reactive Oxygen Species (ROS) Apoptosis Cuproptosis	Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Vitisin A ((+)-Vitisin A) is an orally active natural product with multiple pharmacological activities including anti-inflammatory, anti-tumor, anti-oxidant, anti-pathogenic microorganism, hypoglycemic and lipid-regulating, anti-osteoporotic, neuroprotective and cardiovascular protective effects. Vitisin A exhibits inhibitory effects on human AChE and MAO-B with IC₅₀ values of 1.29 µM and 4.94 µM, respectively. Vitisin A inhibits the ERK, MAPK, NF-κB, STAT1, HMGCR and TRAF6 pathways, downregulates the related phosphorylation and protein expression, while activates the Nrf2/HO-1 pathway and upregulates p21 expression. Vitisin A induces tumor cell apoptosis and cell cycle arrest, inhibits adipogenesis and lipid accumulation, while alleviates oxidative stress, suppresses inflammatory responses, blocks hepatic fibrosis, Cuproptosis and cholesterol synthesis, and increases the expression levels of central BDNF and TrkB. Vitisin A can be used in the research of tumors, infectious diseases, metabolic diseases, bone and joint diseases, liver diseases, skin injuries, as well as neurodegenerative and cognitive dysfunction-related diseases .

HY-175649

LATS1/2-IN-1	Large Tumor Suppressor (LATS) YAP	Cancer
LATS1/2-IN-1 is a potent and selective LATS1 and LATS2 inhibitor. LATS1/2-IN-1 exhibits potent inhibitory activity against LATS1 and LATS2 with IC₅₀ values of 4.4 nM and 5.5 nM as determined via r ³³P functional assay. LATS1/2-IN-1 displays cellular IC₅₀ values of 136 nM for LATS1 and 36.0 nM for LATS2 as determined via NanoBRET assay. LATS1/2-IN-1 reduces phosphorylation of YAP1 in mouse liver. LATS1/2-IN-1 demonstrates wound healing activity in HT-1080 scratch assay and in vivo SKH1 mouse punch biopsy model. LATS1/2-IN-1 can be used for the study of regenerative medicine indications such as wound healing .

HY-118528A

TP0427736 hydrochloride 2 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-P11358

IRW	Angiotensin-converting Enzyme (ACE) Acetyl-CoA Carboxylase Mitochondrial Metabolism	Inflammation/Immunology
IRW is an orally active tripeptide produced from egg white with angiotensin converting enzyme (ACE) inhibitory properties. IRW can prevent high-fat diet (HFD)-induced Non-alcoholic fatty liver disease (NAFLD) by modulating hepatic lipid metabolism and increasing mitochondrial content. IRW decreases hepatic triglyceride content and lipid droplet size. IRW increases the hepatic mitochondrial complexes and citrate synthase activity, phosphorylation of 5’-AMP-activated protein kinase and microsomal triglyceride transfer protein abundance. IRW increases phosphorylated acetyl CoA carboxylase and mitochondrial complexes, IRW can be used for the research of inflammation .

HY-177780

Cyclin K degrader 2	Molecular Glues CDK Apoptosis	Cancer
Cyclin K degrader 2 is a molecular glucose degrading agent that targets the cyclin K protein. Cyclin K degrader 2 has inhibitory activity against CDK1 and CDK9. Cyclin K degrader 2 causes a decrease in RNA polymerase II Ser2 phosphorylation levels, downregulation of DNA damage response gene expression, accumulation of DNA damage, G1 phase arrest of the cell cycle, and apoptosis. Cyclin K degrader 2 can be used for cancer research .

HY-117710B

AD-35	Cholinesterase (ChE) Amyloid-β ERK TNF Receptor Interleukin Related	Neurological Disease
AD-35 is an orally active anti-Alzheimer's disease (AD) agent with moderate AChE inhibitory activity and metal ion chelating ability. AD-35 exhibits IC₅₀ values for AChE and BuChE of 793 nM and 31428 nM, respectively. AD-35 can form chelates with Cu²⁺ and Fe³⁺, but its chelating ability for Zn²⁺ is relatively weak. AD-35 can inhibit Aβ aggregation and disassemble the formed Aβ aggregates, and inhibit Aβ-induced ERK phosphorylation. AD-35 inhibits neuroinflammation in AD rat models and demonstrates a strong effect in improving cognitive function .

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-143884

JAK2/TYK2-IN-1 1 Publications Verification	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-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-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-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-105369

KF-20444	Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies .

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 .

HY-178448

EGFR-IN-178	EGFR JAK Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Cannabinoid Receptor Glutathione Peroxidase Caspase	Inflammation/Immunology Cancer
EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC₅₀ = 3.4 nM), L858R/T790 M (IC₅₀ = 2.9 nM), and Del19/T790 M (IC₅₀ = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC₅₀ = 55.6 nM) and JAK3 (IC₅₀ = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC) .

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-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-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-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-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-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-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-137381

6-Bnz-cAMP N6-Benzoyl-cAMP	PKA Potassium Channel	Metabolic Disease
6-Bnz-cAMP, a derivative of cyclic adenosine monophosphate (cAMP), is a selective PKA activator with inhibitory activity against the bTREK-1 K ⁺ channel. 6-Bnz-cAMP does not activate the Epac signaling pathway. 6-Bnz-cAMP inhibits the bTREK-1 K ⁺ channel via a voltage-independent, ATP-dependent mechanism that is independent of the PKA/Epac/calmodulin kinase/MAP kinase pathway. 6-Bnz-cAMP activates CREB phosphorylation to regulate osteoblast-specific gene expression, induces osteoblast differentiation, promotes extracellular matrix mineralization, supports osteoblast proliferation, and shows no cytotoxicity toward osteoblasts. 6-Bnz-cAMP can be used in studies related to bone tissue repair and regeneration .

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-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-181912

D-DT/MIF-1-IN-1	Macrophage migration inhibitory factor (MIF) ERK	Cancer
D-DT/MIF-1-IN-1 (Compound 4h) is a non-competitive, non-covalent inhibitor of MIF-1 and D-DT, with IC₅₀ values of 2.4 μM and 4.0 μM against D-DT, and an IC₅₀ value of 9.8 μM against MIF-1. D-DT/MIF-1-IN-1 inhibits D-DT-induced phosphorylation of ERK and exerts antiproliferative activity in non-small cell lung cancer cells .

HY-402805

DYRK2-IN-2	DYRK CDK Tau Protein	Cancer
DYRK2-IN-2 (Compound C17) is a selective inhibitor of DYRK2, with its IC₅₀ value being 40.3 nM. The inhibitory activity of DYRK2-IN-2 on DYRK1A (IC₅₀ = 1842 nM), DYRK1B (IC₅₀ = 1335 nM), DYRK4 (IC₅₀ = 1931 nM), DYRK3 (IC₅₀ = 112 nM), and CLKs (IC₅₀ = 540-6496 NM) is relatively low. DYRK2-IN-2 inhibits the phosphorylation of Tau protein at Thr212 and shows moderate cytotoxicity in HT22 cells. DYRK2-IN-2 can be used in cancer research .

HY-180956

PROTAC ALK degrader-5	PROTACs Anaplastic lymphoma kinase (ALK) STAT	Cancer
PROTAC ALK degrader-5 (Compound 17) is an efficient ALK PROTAC degrader, with its inhibitory effects on EML4-ALK and NPM-ALK being 27.4 nM and 116.5 nM respectively. PROTAC ALK degrader-5 exhibits potent anti-proliferative activity against H3122 and Karpas 299. PROTAC ALK degrader-5 effectively inhibits the phosphorylation of ALK and STAT3. PROTAC ALK degrader-5 can be used for the study of ALK-driven malignant tumors, such as human non-small cell lung cancer and anaplastic large cell lymphoma .

HY-181800

SHP2-IN-47	SHP2 Akt ERK Apoptosis	Cancer
SHP2-IN-47 is a selective and potent SHP2 inhibitor with an IC₅₀ of 0.80 μM. SHP2-IN-47 exhibits potent inhibitory activity against SHP2 ^E76K(IC₅₀ = 0.37 μM). SHP2-IN-47 functionally inhibits protein tyrosine phosphatase domains and downregulates SHP2-mediated phosphorylation of AKT and ERK. SHP2-IN-47 induces apoptosis and suppresses proliferation of cancer cells. SHP2-IN-47 can be used for the research of cancer, such as acute myelocytic leukemia .

HY-181031

FGFR-IN-24	FGFR Apoptosis Akt p38 MAPK	Cancer
FGFR-IN-24 (Compound 8r) is a FGFR inhibitor. FGFR-IN-24 potently inhibits FGFR1/2/3 with IC₅₀ values of 10.0, 6.9, and 30.2 nM, respectively. FGFR-IN-24 exhibits superior inhibitory activity toward FGFR1 ^V561M, FGFR2 ^V564F, and FGFR2 ^N549K mutations with IC₅₀ values of 6.8, 0.7, and 0.8 nM, respectively. FGFR-IN-24 induces Apoptosis. FGFR-IN-24 efficiently suppresses the phosphorylation of FGFR2 and its downstream signaling mediators (AKT and MAPK). FGFR-IN-24 demonstrates favorable antitumor efficacy in an RT112/84 bladder cancer xenograft model .

HY-100754R

Ritlecitinib (Standard) PF-06651600 (Standard)	JAK Reference Standards Interleukin Related STAT	Inflammation/Immunology
Ritlecitinib (Standard) is the analytical standard of Ritlecitinib (HY-100754). This product is intended for research and analytical applications. 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-182788

Multitarget AD-IN-7	GSK-3 Tau Protein Amyloid-β β-catenin	Neurological Disease
Multitarget AD-IN-7 is an orally active multi-target anti-AD compound. Multitarget AD-IN-7 exhibits inhibitory activity against GSK-3β and GSK-3α (IC₅₀ = 0.66, 0.83 nM). Multitarget AD-IN-7 upregulates the expression of p-GSK-3β-Ser9, inhibits the phosphorylation of tau-Ser396, targets Aβ_1-42, chelates pathogenic metal ions, scavenges ABTS•+, upregulates the expression of β-catenin and neurogenesis biomarkers, and promotes neurite outgrowth. Multitarget AD-IN-7 improves motor ability in Alzheimer's disease zebrafish. Multitarget AD-IN-7 is applicable to research related to Alzheimer's disease .

HY-182368

PI3Kα-IN-30	PI3K Akt Apoptosis	Cancer
PI3Kα-IN-30 is an orally active, selective PI3Kα inhibitor with an IC₅₀ of 2.8 nM. PI3Kα-IN-30 inhibits cancer cell proliferation, as well as the phosphorylation of Akt (S473) and pS6 (S240/244). PI3Kα-IN-30 shows low growth inhibitory activity against normal somatic cell lines at a concentration of 30 μM. PI3Kα-IN-30 induces cancer cell apoptosis and exerts anti-tumor efficacy in xenograft models. PI3Kα-IN-30 can be used for the research of breast cancer .

Cat. No.	Product Name	Target	Research Area