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ATP binding site

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (2) Apoptosis (4) Autophagy (2) Bacterial (3) Bcr-Abl (2) BCRP (1) Btk (1) c-Kit (2) Casein Kinase (1) CDK (1) Cholinesterase (ChE) (1) Drug Metabolite (1) EGFR (5) Eukaryotic Initiation Factor (eIF) (1) GSK-3 (2) HSP (2) IRE1 (2) MAP3K (1) MEK (1) Microtubule/Tubulin (1) p97 (1) Parasite (1) PDGFR (2) PDHK (1) PI3K (2) PI4K (1) Potassium Channel (1) Raf (1) ROS Kinase (1) SARS-CoV (2)
By Research Areas:	Cancer (19) Infection (3) Inflammation/Immunology (4) Metabolic Disease (1) Neurological Disease (2)

Inhibitors & Agonists

Fluorescent Dye

Isotope-Labeled Compounds

Targets Recommended: ATP Synthase ATP Citrate Lyase Penicillin-binding protein (PBP) FKBP FABP Transthyretin (TTR) Ligands for Target Protein for PROTAC P-glycoprotein YB-1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12062

PD318088 1 Publications Verification	MEK	Cancer
PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research .

HY-160519

Targocil-II	Bacterial Antibiotic	Infection
Targocil-II (Compound 2) is an ABC transporter inhibitor with a IC₅₀ value of 137 nM. Targocil-II prevents ATP hydrolysis by binding to allosteric sites of the TM domain. Targocil-II has (antibacterial) activity .

HY-107578

Macbecin Macbecin I; NSC 330499	HSP	Cancer
Macbecin is a stable HSP90 inhibitor by binding to the ATP-binding site with an IC₅₀ of 2 μM and a K_d of 0.24 μM. Macbecin exhibits antitumor and cytocidal activities .

HY-160564

ZNL-0056	EGFR	Cancer
ZNL-0056 is an orally active *ATP-competitive* inhibitor that targets both the Cys797 and Cys775 in the ATP binding site of EGFR. ZNL-0056 selectively inhibits EGFR and its downstream signaling in H3255 cells. ZNL-0056 can be used for the research of cancer .

HY-146801

PDHK-IN-3	PDHK	Metabolic Disease Cancer
PDHK-IN-3 (compound 7) is a potent PDHK (pyruvate dehydrogenase kinase) inhibitor, with IC₅₀ values of 0.21 and 1.54 μM for PDHK2 and PDHK4, respectively .

HY-157508

VCP Activator 1	p97	Others
VCP Activator 1 is a VCP activator that dose-dependently stimulates VCP ATPase activity. VCP Activator 1 binds an allosteric pocket near the C-terminus. In addition, VCP Activator 1 binding site can also be occupied by a phenylalanine residue in the VCP C-terminal tail .

HY-153761

ASK1-IN-4

MAP3K Apoptosis Inflammation/Immunology Cancer

ASK1-IN-4 (Compound 17) is an ASK1 inhibitor (IC₅₀=0.2 μM). ASK1-IN-4 interacts with ATP-binding site of ASK1 .

ASK1-IN-4	MAP3K Apoptosis	Inflammation/Immunology Cancer
ASK1-IN-4 (Compound 17) is an ASK1 inhibitor (IC₅₀=0.2 μM). ASK1-IN-4 interacts with ATP-binding site of ASK1 .

HY-155941

5-Hydroxydecanoic acid	Potassium Channel	Neurological Disease
5-Hydroxydecanoic acid (5-HD） is a K_ATP channel antagonist，which has the effect of blocking the K K_ATP channel only during ischaemia by competing with the ATP binding site and does not affect pancreatic K_ATP channels .

HY-110079

TNP	Others	Cancer
TNP is a cell-permeable inhibitor of IP6K1 and IP3K, with IC₅₀ values of 0.55 µM and 10.2 µM for IP3K, respectively. TNP binds to the ATP-binding sites of both enzymes .

HY-115749

D-Luciferin 6′-methyl ether 6′-Methoxyluciferin	Others	Others
D-Luciferin 6′-methyl ether (6′-Methoxyluciferin; compound 19a) is a potent luciferase from the North American firefly Photinus pyralis (PpyLuc) inhibitor with an IC₅₀ of 0.1 µM. D-Luciferin 6′-methyl ether, a D-luciferin analog, shows non-specific interactions at ATP- and luciferin-binding sites of the PpyLuc active site .

HY-145425

PAIR2	IRE1	Cancer
PAIR2 is a potent and selective partial antagonist of IRE1α RNase. PAIR2 can completely occupy IRE1α’s ATP-binding site in cells and block the ability of a potent KIRA to inhibit XBP1 splicing .

HY-112299

Zipalertinib 1 Publications Verification TAS6417; CLN-081	EGFR Apoptosis	Cancer
Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC₅₀ values ranging from 1.1-8.0 nM .

HY-118773

MreB Perturbing Compound A22 hydrochloride A22 hydrochloride	Bacterial Antibiotic	Inflammation/Immunology
MreB Perturbing Compound A22 hydrochloride is a benzylisothiourea compound that interacts with the ATP binding site of MreB rapidly and reversibly. MreB Perturbing Compound A22 hydrochloride blocks normal rod shape formation and inhibits chromosome partitioning in E. coli, inhibiting growth (MIC=3.1 µg/ml).

HY-17547

NMS-E973 2 Publications Verification	HSP	Cancer
NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC₅₀ of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy .

HY-145422

KIRA9	IRE1 Apoptosis	Others
KIRA9 is a potent IRE1 inhibitor (IC₅₀=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis .

HY-18010

PCI 29732 3 Publications Verification	Btk BCRP	Inflammation/Immunology
PCI 29732 is a potent, orally active, reversible BTK inhibitor with K_i ^app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 .

HY-10261B

(E/Z)-Afatinib (E/Z)-BIBW 2992
(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells .

HY-15463

Imatinib Maximum Cited Publications 69 Publications Verification STI571; CGP-57148B	Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy	Cancer
Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .

HY-149846

SIQ17	EGFR	Cancer
SIQ17 is an EGFR inhibitor that inhibits its activity by occupying the ATP-binding site, with IC₅₀ of 0.62 nM. SIQ17 shows more effective EGFR-TK inhibitory activity compared to the known inhibitor Erlotinib (HY-50896) (IC₅₀ of ∼20 nM). SIQ17 can be used for cancer research

HY-128778

DBPR112	EGFR	Cancer
DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC₅₀s of 15 nM and 48 nM for EGFR ^WT and EGFR ^L858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy .

HY-149292

SR-4133	Casein Kinase	Cancer
SR-4133 is a potent and highly CK1ε selective inhibitor with an IC₅₀ of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1 .

HY-15463S2

Imatinib-d3 hydrochloride STI571-d₃ hydrochloride; CGP-57148B-d₃ hydrochloride	Autophagy Bcr-Abl c-Kit SARS-CoV PDGFR	Cancer
Imatinib-d₃ (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.

HY-131275

Imatinib Impurity E	Drug Metabolite	Others
Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .

HY-111930

5-Iodo-indirubin-3'-monoxime	GSK-3 CDK	Cancer
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC₅₀s of 9, 20 and 25 nM, respectively .

HY-101562

Inavolisib 2 Publications Verification GDC-0077; RG6114	PI3K Apoptosis	Cancer
GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC₅₀=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα .

HY-106005

MMV390048 2 Publications Verification	Parasite PI4K	Infection
MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (K_d ^app=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent .

HY-100848

TX1-85-1 1 Publications Verification	EGFR	Cancer
TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC₅₀ of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling .

HY-107779

BI-882370	Raf	Cancer
BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAF ^V600E-mutant, the WT BRAF and CRAF kinases with IC₅₀s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases .

HY-144381

Glutamate-5-kinase-IN-1	Bacterial	Infection
Glutamate-5-kinase-IN-1 (compound 50) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.1 µM. Glutamate-5-kinase-IN-1 shows G5K inhibition by alters the ATP binding site architecture for enzyme recognition. Glutamate-5-kinase-IN-1 has the potential for the research of anti-TB agents .

HY-101513

eIF4A3-IN-1 3 Publications Verification	Eukaryotic Initiation Factor (eIF)	Cancer
eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC₅₀=0.26 μM; K_d=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD .

HY-155975

PI3Kδ-IN-14	PI3K	Inflammation/Immunology
PI3Kδ-IN-14 (Compound (S)-29) is a selective PI3Kδ inhibitor (IC₅₀: 0.8 nM, K_d: 84.8 nM). PI3Kδ-IN-14 binds to the ATP-binding site of the kinase domain of PI3Kδ. PI3Kδ-IN-14 has anti-inflammatory activity by inhibiting the PI3K/AKT pathway. PI3Kδ-IN-14 ameliorates acute lung injury (ALI) .

HY-150537

AChE/GSK-3β-IN-1	Cholinesterase (ChE) GSK-3 Microtubule/Tubulin ROS Kinase	Neurological Disease
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC₅₀ values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research .

(Rac)-Luciferin 6′-methyl ether sodium (Rac)-6′-Methoxyluciferin sodium	Fluorescent Dyes/Probes
D-Luciferin 6′-methyl ether (6′-Methoxyluciferin; compound 19a) sodium is a potent luciferase from the North American firefly Photinus pyralis (PpyLuc) inhibitor with an IC₅₀ of 0.1 μM. D-Luciferin 6′-methyl ether, a D-luciferin analog, shows non-specific interactions at ATP- and luciferin-binding sites of the PpyLuc active site .

Imatinib-d3 hydrochloride
Imatinib-d₃ (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.

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