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Results for "

ATP-pocket

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (7) ATM/ATR (1) Autophagy (4) Bacterial (1) Biochemical Assay Reagents (1) CDK (3) Checkpoint Kinase (Chk) (2) DNA/RNA Synthesis (2) DYRK (2) EGFR (2) Eukaryotic Initiation Factor (eIF) (1) FGFR (1) Interleukin Related (1) IRAK (1) JNK (1) mTOR (1) Necroptosis (1) Organoid (4) p38 MAPK (4) PKA (1) Pyruvate Kinase (1) Reference Standards (3) RIP kinase (2) Survivin (1) TAM Receptor (1) TGF-β Receptor (2) TNF Receptor (1) VEGFR (1)
By Research Areas:	Cancer (14) Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (8) Neurological Disease (5)

By Targets:

Apoptosis (7)

ATM/ATR (1)

Autophagy (4)

Bacterial (1)

Biochemical Assay Reagents (1)

CDK (3)

Checkpoint Kinase (Chk) (2)

DNA/RNA Synthesis (2)

DYRK (2)

EGFR (2)

Eukaryotic Initiation Factor (eIF) (1)

FGFR (1)

Interleukin Related (1)

IRAK (1)

JNK (1)

mTOR (1)

Necroptosis (1)

Organoid (4)

p38 MAPK (4)

PKA (1)

Pyruvate Kinase (1)

Reference Standards (3)

RIP kinase (2)

Survivin (1)

TAM Receptor (1)

TGF-β Receptor (2)

TNF Receptor (1)

VEGFR (1)

By Research Areas:

Cancer (14)

Cardiovascular Disease (1)

Infection (1)

Inflammation/Immunology (8)

Neurological Disease (5)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10295

SB 202190 Maximum Cited Publications 134 Publications Verification	Organoid p38 MAPK Autophagy Apoptosis	Neurological Disease Cancer
SB 202190 is a selective p38 MAP kinase inhibitor with IC₅₀s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a K_d of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits . SB202190 induces autophagy .

HY-157941

ART0380	ATM/ATR Checkpoint Kinase (Chk) DNA/RNA Synthesis	Cancer
ART0380 is a potent, selective and orally active ATR kinase inhibitor. ART0380 potently inhibits human ATR-ATRIP complex with an IC₅₀ of 51.7 nM. ART0380 binds the ATP pocket of the ATR-ATRIP complex, blocks ATR-dependent Chk1 serine 345 phosphorylation, and induces cell cycle disorder and DNA damage. ART0380 demonstrates potent and selective antitumor activity in preclinical models with varying types of ataxia-telangiectasia mutated (ATM) gene aberrancy. ART0380 can be used for the research of cancer, such as colorectal cancer and prostate cancer .

HY-108476

INDY 2 Publications Verification	DYRK	Cancer
INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC₅₀s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a K_i value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells .

HY-125510

UNC2541 1 Publications Verification	TAM Receptor	Neurological Disease Inflammation/Immunology
UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor, binds in the MerTK ATP pocket, with an IC₅₀ of 4.4 nM, more selective over Axl, Tyro3 and Flt3. UNC2541 inhibits phosphorylated MerTK (pMerTK; EC₅₀, 510 nM). UNC2541 abolishes the analgesic and anti-inflammatory effects of ozone in vivo and in vitro .

HY-10295A

SB 202190 hydrochloride Maximum Cited Publications 134 Publications Verification	Organoid p38 MAPK Autophagy Apoptosis	Neurological Disease Cancer
SB 202190 hydrochloride is a selective p38 MAP kinase inhibitor with IC₅₀s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 hydrochloride binds to the ATP pocket of the active recombinant human p38 kinase with a K_d of 38 nM. SB 202190 hydrochloride has anti-cancer activity . SB202190 hydrochloride induces autophagy .

HY-N5112A

β,β-Dimethylacrylalkannin 3 Publications Verification Arnebin 1	FGFR Necroptosis Apoptosis CDK JNK	Inflammation/Immunology
β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC₅₀=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .

HY-N4148

Purpureaside C	DNA/RNA Synthesis Apoptosis Bacterial	Infection Inflammation/Immunology Cancer
Purpureaside C, phenolic glycoside, is a minichromosome maintenance complex component 6 (MCM6) inhibitor. Purpureaside C binds to the ATP-pocket of MCM6, suppresses MCM6 protein expression in gastric cancer cells. Purpureaside C suppresses gastric cancer cell growth and induces apoptosis. Purpureaside C exerts antibacterial activity and proinflammatory activity. Purpureaside C can be used for the researches of gastric cancer, bacterial infection and inflammation .

HY-W319647

GCN2 activator-1	Eukaryotic Initiation Factor (eIF) Pyruvate Kinase	Inflammation/Immunology
GCN2 activator-1 (Compound 20) is a GCN2 activator. GCN2 activator-1 binds within the ATP-pocket of GCN2 and activates GCN2 in a GCN1-independent manner. GCN2 activator-1 activates Integrated Stress Response (ISR) in cells. GCN2 activator-1 inhibits PKR with an IC₅₀ of 3.75 µM. GCN2 activator-1 can be used for research of pulmonary veno-occlusive disease (PVOD) .

HY-19628

OD36	RIP kinase TGF-β Receptor	Inflammation/Immunology
OD36 is a RIPK2 inhibitor with an IC₅₀ of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 shows ALK2-directed activity with K_Ds of 37 nM .

HY-138916

PF-06672131	Biochemical Assay Reagents EGFR	Others
PF-06672131 is an alkynylated afatinib derivative and a small molecule probe that is reactive to cysteine. PF-06672131 is an inhibitor of epidermal growth factor receptor (EGFR) kinase that targets the *ATP* pockets of EGFR. PF-06672131 can be used for activity-based protein profiling studies .

HY-123045

PNU-292137	CDK	Cancer
PNU-292137 is an orally active, potent CDK2 inhibitor with IC₅₀s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model .

HY-19628A

OD36 hydrochloride	RIP kinase TGF-β Receptor	Inflammation/Immunology
OD36hydrochloride is a RIPK2 inhibitor with an IC₅₀ of 5.3 nM. OD36 hydrochloride is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 hydrochloride shows ALK2-directed activity with K_Ds of 37 nM .

HY-159707

MCL1020	Checkpoint Kinase (Chk)	Cardiovascular Disease Cancer
MCL1020 is a CHK1 inhibitor with an IC₅₀ of 1.61 μM. MCL1020 properly occupies the ATP pocket by interacting with a diverse range of the sites of CHK1 kinase. MCL1020 can be used for the study of hematologic malignancies .

HY-117622

ND-2110	IRAK	Inflammation/Immunology Cancer
ND-2110 is a selective IRAK4 inhibitor (K_i: 7.5 nM). ND-2110 binds to the ATP pocket of IRAK4. ND-2110 targets the subset of activated B cell-like (ABC) subtype of diffuse large B cell lymphoma (DLBCL) cell lines with MYD88 L265P mutations,. ND-2110 inhibits LPS-induced TNF production, alleviates collagen-induced arthritis, and blocks gout formation in mouse models .

HY-N12399

Aplithianines A	PKA	Inflammation/Immunology
Aplithianines A is a potent inhibitor against J-PKA_cα with an IC₅₀ of 1 μM , and inhibits wild-type PKA with an IC₅₀ of 84 nM. Aplithianines A inhibits J-PKAcα catalytic activity by competitively binding to the *ATP* pocket .

HY-18953

mTOR inhibitor-23	mTOR	Cancer
mTOR inhibitor-23 (compound DHM25) is a selective, competitive, irreversible and covalent inhibitor of mTOR. mTOR inhibitor-23 has the mechanism of inhibition occurs mainly through its capacity to covalently interact with a nucleophilic amino acid inside the ATP pocket. mTOR inhibitor-23 exerts potent antitumor activity against triple-negative breast tumor cell lines .

HY-160687

GW549390X	VEGFR	Others
GW549390X is a dual inhibitor of Fluc and VEGFR2 with IC₅₀ of 0.26 μM and 1.2 μM, respectively. GW549390X can bind to the ATP pocket of FLuc through the aniline side chain and is an ATP-competitive inhibitor of Fluc. GW549390X acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases, with potential implications for Fluc reporter assays .

HY-10295AR

SB 202190 hydrochloride (Standard)	Organoid Reference Standards p38 MAPK Autophagy Apoptosis	Neurological Disease Cancer
SB 202190 (hydrochloride) (Standard) is the analytical standard of SB 202190 (hydrochloride). This product is intended for research and analytical applications. SB 202190 hydrochloride is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 hydrochloride binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 hydrochloride has anti-cancer activity . SB202190 hydrochloride induces autophagy .

HY-10295R

SB 202190 (Standard)	Organoid Reference Standards p38 MAPK Autophagy Apoptosis	Neurological Disease Cancer
SB 202190 (Standard) is the analytical standard of SB 202190. This product is intended for research and analytical applications. SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits . SB202190 induces autophagy .

HY-108476R

INDY (Standard)	Reference Standards DYRK	Cancer
INDY (Standard) is the analytical standard of INDY (HY-108476). This product is intended for research and analytical applications. INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC₅₀s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a K_i value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells .

HY-118447

RO0505124	CDK Survivin	Cancer
RO0505124 is a selective CDK4 inhibitor with an IC₅₀ of 20 nM. RO0505124 reversibly binds the ATP pocket of the kinase. RO0505124 induces G1 phase arrest in cancer cells via reduced retinoblastoma protein (Rb) phosphorylation, blocking S phase progression. RO0505124 exhibits anti-proliferative activity against various cancer cells. RO0505124 delays mitotic entry, induces aberrant mitosis with lagging chromosomes, driving mitotic slippage and formation of multinucleated or micronucleated cells. RO0505124 inhibits G2/M phase accumulation of survivin and borealin. RO0505124 can be used for the research of cancer .

HY-181657

EGFR-IN-200	EGFR TNF Receptor Interleukin Related Apoptosis	Cancer
EGFR-IN-200 is an inhibitor targeting EGFR, TNF-α, and the IL-6/GP130 complex, which potently targets human EGFR (IC₅₀=0.03 μM), TNF-α (IC₅₀=3.1 μM), and the IL-6/GP130 complex (IC₅₀=1.6 μM). EGFR-IN-200 binds to the ATP pocket of EGFR, the trimer interface of TNF-α, and the cytokine-receptor interface of IL-6/GP130, induces G₂/M cell cycle arrest, apoptosis, and antiproliferative activity. EGFR-IN-200 exhibits high gastrointestinal absorbability, low BBB permeability, and complies with the Lipinski's rule. EGFR-IN-200 can be used for the research of lung cancer and breast adenocarcinoma .

Cat. No.	Product Name

HY-L158

Highly Selective Inhibitors Library	6,135 compounds
According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 6,135 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes

Highly Selective Inhibitors Library

6,135 compounds

According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 6,135 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes

β,β-Dimethylacrylalkannin 3 Publications Verification Arnebin 1	Quinones Structural Classification other families Classification of Application Fields Other Diseases Plants Naphthalene Quinones Pteris livida Mett. Disease Research Fields	FGFR Necroptosis Apoptosis CDK JNK
β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC₅₀=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .

Purpureaside C	Structural Classification Classification of Application Fields Simple Phenylpropanols Phenols Polyphenols Scrophulariaceae Phenylpropanoids Plants Rehmannia glutinosa (Gaert.) Libosch. ex Fisch. et Mey Inflammation/Immunology Disease Research Fields Source Classification	DNA/RNA Synthesis Apoptosis Bacterial
Purpureaside C, phenolic glycoside, is a minichromosome maintenance complex component 6 (MCM6) inhibitor. Purpureaside C binds to the ATP-pocket of MCM6, suppresses MCM6 protein expression in gastric cancer cells. Purpureaside C suppresses gastric cancer cell growth and induces apoptosis. Purpureaside C exerts antibacterial activity and proinflammatory activity. Purpureaside C can be used for the researches of gastric cancer, bacterial infection and inflammation .

Aplithianines A	Alkaloids Microorganisms Other Alkaloids Source Classification	PKA
Aplithianines A is a potent inhibitor against J-PKA_cα with an IC₅₀ of 1 μM , and inhibits wild-type PKA with an IC₅₀ of 84 nM. Aplithianines A inhibits J-PKAcα catalytic activity by competitively binding to the *ATP* pocket .

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