Search Result
Results for "
ATP binding site
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-12062
-
|
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
-
|
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-157508
-
|
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-107578
-
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 Kd of 0.24 μM. Macbecin exhibits antitumor and cytocidal activities .
|
-
-
- HY-146801
-
|
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-160564
-
|
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-153761
-
-
-
- HY-155941
-
|
Potassium Channel
|
Neurological Disease
|
5-Hydroxydecanoic acid (5-HD) is a KATP channel antagonist,which has the effect of blocking the K KATP channel only during ischaemia by competing with the ATP binding site and does not affect pancreatic KATP channels .
|
-
-
- HY-110079
-
|
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-100214
-
|
EGFR
|
Cancer
|
EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFR L858R/T790M. EAI001 can be used for research of cancer .
|
-
-
- HY-115749
-
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
-
|
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
-
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
-
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
-
|
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
-
|
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
-
|
Btk
BCRP
|
Inflammation/Immunology
|
PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki 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)-BIBW 2992
|
EGFR
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
Autophagy
|
Others
|
(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
71 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
-
|
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
-
|
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
-
|
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
-
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
-
|
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
-
|
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
-
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-10261BR
-
|
EGFR
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
Autophagy
|
Others
|
(E/Z)-Afatinib (Standard) is the analytical standard of (E/Z)-Afatinib. This product is intended for research and analytical applications. (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-15463R
-
|
|
Cancer
|
Imatinib (Standard) is the analytical standard of Imatinib. This product is intended for research and analytical applications. 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-P10280
-
|
ATM/ATR
|
Cancer
|
ATR kinase substrate peptide (compound 45) is a potent and selective inhibitor of ATR (Ataxia Telangiectasia and Rad3 related) protein kinase (Ki=6 nM). ATR kinase substrate peptide inhibits ATR activity by competing with ATR kinase ATP-binding sites to block ATR mediated signaling. ATR kinase substrate peptide can be used to study the role of ATR kinase in DNA damage response .
|
-
-
- HY-106005
-
|
Parasite
PI4K
|
Infection
|
MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kd 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
-
|
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
-
|
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
-
|
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
-
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=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
-
|
PI3K
|
Inflammation/Immunology
|
PI3Kδ-IN-14 (Compound (S)-29) is a selective PI3Kδ inhibitor (IC50: 0.8 nM, Kd: 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
-
|
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 .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-115749A
-
(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 .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10280
-
|
ATM/ATR
|
Cancer
|
ATR kinase substrate peptide (compound 45) is a potent and selective inhibitor of ATR (Ataxia Telangiectasia and Rad3 related) protein kinase (Ki=6 nM). ATR kinase substrate peptide inhibits ATR activity by competing with ATR kinase ATP-binding sites to block ATR mediated signaling. ATR kinase substrate peptide can be used to study the role of ATR kinase in DNA damage response .
|
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-15463S2
-
|
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.
|
-
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: