Search Result
Results for "
ATP-binding site
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-15463
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Imatinib
Maximum Cited Publications
120 Publications Verification
STI571; CGP-57148B
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Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
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Cancer
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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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- HY-101562
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GDC-0077; RG6114
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PI3K
Apoptosis
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Cancer
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Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer .
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- HY-128933
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Adenylyl-imidodiphosphate tetralithium
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Potassium Channel
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Metabolic Disease
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AMP-PNP (Adenylyl-imidodiphosphate) tetralithium is a non-hydrolyzable ATP analog. AMP-PNP tetralithium binds to ATP binding sites competely but is not hydrolyzed by enzymes, providing stable experimental conditions for studying ATP-dependent processes. AMP-PNP tetralithium can also be used to study enzyme activity, kinase regulation, DNA/RNA metabolism, ion channel function, and protein complex assembly .
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- HY-112299
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TAS6417; CLN-081
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EGFR
Apoptosis
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Cancer
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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 .
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- HY-130777A
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Adenylyl imidodiphosphate lithium hydrate
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Drug Derivative
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Metabolic Disease
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AMP-PNP (Adenylyl imidodiphosphate) lithium hydrate is a non-hydrolyzable ATP analog. AMP-PNP lithium hydrate binds to ATP binding sites competely but is not hydrolyzed by enzymes, providing stable experimental conditions for studying ATP-dependent processes. AMP-PNP lithium hydrate can also be used to study enzyme activity, kinase regulation, DNA/RNA metabolism, ion channel function, and protein complex assembly .
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- HY-101513
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Eukaryotic Initiation Factor (eIF)
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Neurological Disease
Cancer
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eIF4A3-IN-1 is a selective eIF4A3 inhibitor (IC50: 0.26 μM; Kd: 0.043 μM) with cellular nonsense-mediated RNA decay (NMD) inhibitory activity. eIF4A3-IN-1 can specifically bind to the non-ATP binding site of eIF4A3. eIF4A3-IN-1 has anti-tumor and analgesic activities .
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- HY-100848
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EGFR
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Cancer
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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 .
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- HY-159520
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Ofirnoflast; HT-6184
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NEKs
NOD-like Receptor (NLR)
Caspase
Apoptosis
Pyroptosis
NF-κB
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC50 of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia .
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- HY-10261B
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(E/Z)-BIBW 2992
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EGFR
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
Autophagy
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Others
Cancer
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(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 .
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- HY-106005
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Parasite
PI4K
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Infection
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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 .
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- HY-17547
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HSP
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Cancer
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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 .
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- HY-12062
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MEK
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Cancer
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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 .
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- HY-107779
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Raf
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Cancer
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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 .
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- HY-110079
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IPK Superfamily
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Cancer
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TNP is a competitive, reversible inhibitor of IP6K1 and IP3K, with IC50s of 0.55 μM and 10.2 μM for IP6K1 and IP3K, respectively. TNP competitively binds to the ATP binding site of IP6K, inhibits the generation of 5-IP7, and thus relieves the inhibition of 5-IP7 on the AKT signaling pathway. TNP can enhance insulin sensitivity and promote thermogenesis in adipose tissue. TNP cannot effectively pass through the blood-brain barrier and is mainly used in the study of obesity, type 2 diabetes, and metabolic syndrome. However, TNP also inhibits CYP3A4 and may need further optimization[1][2][3].
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- HY-40351
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Drug Intermediate
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Others
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4-Chloro-7H-pyrrolo[2,3-d]pyrimidine is a nitrogen-containing heterocyclic organic synthesis intermediate that can be used for the synthesis of JAK and PKB/Akt inhibitors .
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- HY-12679
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Btk
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Cancer
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PF-06658607 is an alkynylated irreversible Brutons tyrosine kinase (BTK) inhibitor that covalently reacts with active site cysteines in the ATP-binding pocket. PF-06658607 can be used to detect "off "-targets for covalent kinase inhibitors in cancer cells. The alkyne moiety allows for azide-based detection probe via copper-catalyzed click chemistry .
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- HY-156685
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PI4K
Parasite
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Infection
Metabolic Disease
Cancer
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EDI048 is an orally active, gut-restricted parasiticidal agent. EDI048 specifically binds to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocks parasite membrane biogenesis, arrests the pathogen at the schizont stage, and thus irreversibly clears the infection. EDI048 is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, with extremely low systemic exposure, good safety profile, and no cardiotoxicity, genotoxicity or off-target effects. EDI048 is used in studies of intestinal cryptosporidiosis in children .
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- HY-P10280
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ATM/ATR
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Cancer
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ATR kinase substrate peptide (ASELPASQPQPFSAKKK) is a peptide substrate for ATR protein kinase and can be used to detect ATR kinase activity .
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- HY-145425
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IRE1
Apoptosis
FGFR
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Inflammation/Immunology
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PAIR2 is a highly selective inhibitor targeting the kinase domain of human IRE1α, with a Ki value of 8.8 nM against human IRE1α. PAIR2 fully occupies the ATP-binding site of the IRE1α kinase domain, partially antagonizes the ribonuclease activity of IRE1α, specifically inhibits regulated IRE1α-dependent decay (RIDD) and its mediated substrate cleavage, while preserving the splicing function of Xbp1 mRNA. PAIR2 also promotes the differentiation of B cells into plasma cells, blocks IRE1α-induced cell apoptosis, and restores the expression of Fgfr2 mRNA in AT2 cells. PAIR2 effectively reaches a steady-state concentration in the lung tissues of Mus musculus, and serves as an important tool for investigating the function of the IRE1α signaling pathway in diseases such as pulmonary fibrosis .
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- HY-155941
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Potassium Channel
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Neurological Disease
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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 .
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- HY-15463R
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STI571 (Standard); CGP-57148B (Standard)
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Reference Standards
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
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Cancer
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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 .
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- HY-128778
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DBPR112
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EGFR
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Cancer
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Gozanertinib is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFR WT and EGFR L858R/T790M, respectively. Gozanertinib can occupy the ATP-binding site. Gozanertinib has significant antitumor efficacy .
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- HY-18010
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Btk
BCRP
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Inflammation/Immunology
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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 .
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- HY-178980
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Casein Kinase
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Cancer
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APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC50 of 0.348 nM and a Ki of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer .
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- HY-153761
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- HY-164523
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Checkpoint Kinase (Chk)
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Cancer
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PV1162 is a selective Chk2 inhibitor with an IC50 of 0.29 nM. PV1162 inhibits ATP binding to Chk2 by targeting the gatekeeper-dependent hydrophobic pocket, which is specific to Chk2 and located behind the ATP-binding site (adenine-binding region), thereby inhibiting the phosphorylation activity of Chk2. PV1162 holds potential application value in the field of cancer therapy .
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- HY-145422
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IRE1
Apoptosis
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Others
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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 .
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- HY-149292
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Casein Kinase
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Cancer
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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 .
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- HY-120600
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Necroptosis
Apoptosis
RIP kinase
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Inflammation/Immunology
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Sibiriline is a specific competitive inhibitor of RIPK1 that targets the RIPK1 ATP-binding site and locks it in an inactive conformation. Sibiriline inhibits TNF-induced RIPK1-dependent necroptosis and RIPK1-dependent apoptosis, but does not protect cells from caspase-dependent apoptosis. Sibiriline protects mice from concanavalin A-induced hepatitis and has the potential to inhibit immune-dependent hepatitis. .
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- HY-158618
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Aurora Kinase
Apoptosis
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Cancer
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Aurora kinase inhibitor-14 (Compound 79) is an orally active and highly selective inhibitor of Aurora kinases with IC50 values of 0.5 nM and 1.2 nM for Aurora A and Aurora B, respectively. Aurora kinase inhibitor-14 binds to the ATP-binding site of Aurora kinases to block chromosome segregation during mitosis and induce apoptosis in tumor cells. Aurora kinase inhibitor-14 is promising for research of various solid tumors and hematological malignancies, such as non-small cell lung cancer, breast cancer, and acute myeloid leukemia .
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- HY-N11784
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Apoptosis
Caspase
NF-κB
COX
IKK
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Inflammation/Immunology
Cancer
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Triptolidenol, a traditional Chinese medicine, is an epoxy diterpene lactone that can be isolated from Tripterygium wilfordii. Triptolidenol has anti-inflammatory and anticancer activities. Triptolidenol significantly inhibits tumor cell proliferation and migration, arrests cell cycle arrest at S phase and induces apoptosis by activating the cytochrome c/caspase cascade signaling pathway. Triptolidenol disrupts NF-κB/COX-2 pathway by inhibiting IKKβ at ATP-binding sites. Triptolidenol can be used for chronic nephritis and kidney cancer like clear cell renal cell carcinoma (ccRCC) research .
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- HY-161800
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Aminoacyl-tRNA Synthetase
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Infection
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Aminoacyl tRNA synthetase-IN-3 (compound 36K3) is an inhibitor of lysine tRNA synthetase (PfLysRS) from Plasmodium falciparum (IC50=59.2 nM), which inhibits the activity of PfLysRS by occupying the ATP binding site and L-lysine binding site of PfLysRS. Aminoacyl tRNA synthetase-IN-3 can be used in the development of antimalarial drugs .
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- HY-144381
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Bacterial
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Infection
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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 .
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- HY-120622
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Src
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Cancer
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BMS-243117 is a potent, and selective benzothiazole based p56 Lck inhibitor with an IC50 of 4 nM. BMS-243117 inhibits anti-CD3/anti-CD28 induced PBL (human peripheral blood T-cells) proliferation with an IC50 of 1.1 μM. BMS-243117 binds in an extended conformation to the ATP-binding site of Lck .
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- HY-15463S3
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STI571-13C,d3; CGP-57148B-13C,d3
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Isotope-Labeled Compounds
Autophagy
SARS-CoV
Bcr-Abl
PDGFR
c-Kit
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Cancer
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Imatinib- 13C,d3 (STI571- 13C,d3) is 13C 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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- HY-150537
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Cholinesterase (ChE)
GSK-3
Microtubule/Tubulin
ROS Kinase
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Neurological Disease
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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 .
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- HY-12933
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HSP
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Cancer
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BIIB-028 is an orally active inhibitor for heat shock protein 90 (Hsp90). BIIB-028 targets the ATP-binding site of Hsp90, disrupts the function of Hsp90, leads to the degradation of client proteins, that are crucial for cancer cell survival and proliferation .
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- HY-123650
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5'-p-Fluorosulfonylbenzoyladenosine
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Biochemical Assay Reagents
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Cancer
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FSBA (5'-p-Fluorosulfonylbenzoyladenosine) hydrochloride is a covalent modifier and affinity labeling reagent for adenine nucleotide-binding proteins. FSBA hydrochloride covalently attaches to the nucleotide-binding sites of pyruvate kinase, glutamate dehydrogenase, and p56 lck, and to a lysine residue in the ATP-binding site of cAMP-dependent protein kinase, causing loss of enzymatic activity. FSBA hydrochloride can be used for the research of T lymphoma .
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- HY-149846
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EGFR
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Cancer
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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
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- HY-W286614
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Ribosomal S6 Kinase (RSK)
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Inflammation/Immunology
Cancer
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RSK2-IN-4 (Compound 10) is a RSK2 inhibitor, with an inhibition rate of 13.73% on RSK2 activity at 10 μM. RSK2-IN-4 binds to the ATP-binding site of RSK2 in the NTKD (N-terminal kinase domain), with the electron-donating group at the 4-position of the phenyl ring being the key determinant for its inhibitory activity .
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- HY-N15301
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ROCK
Myosin
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Others
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Nocarnickelamide B (Compound 2) is a linear peptide and ROCK1/2 inhibitor. Nocarnickelamide B exhibits dual inhibitory activity against ROCK1 and ROCK2 with IC50s of 14.9 μM and 21.9 μM, respectively. Nocarnickelamide B binds to the ATP-binding site. Nocarnickelamide B inhibits the activation of ROCK-regulated cytoskeletal contraction markers such as the myosin light chain. Nocarnickelamide B is potential for glaucoma reasearch .
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- HY-163726
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GLUT
EGFR
Apoptosis
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Cancer
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GLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of GLUT1 and EGFR. GLUT1/EGFR-IN-1 can simultaneously act on the EGFR tyrosine kinase ATP-binding site and inhibit GLUT1-mediated energy metabolism, resulting in reductions in ATP, MMP, intra-cellular lactic acid, and EGFR nuclear transfer. GLUT1/EGFR-IN-1 can be used for nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC) research .
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- HY-155975
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PI3K
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Inflammation/Immunology
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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) .
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- HY-110333
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EGFR
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Cancer
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BMS-599626 dihydrochloride is a small molecule pan-HER (human epidermal growth factor receptor) kinase inhibitor. BMS-599626 dihydrochloride primarily targets HER1 (IC50=20 nmol/L) and HER2 (IC50=30 nmol/L) kinase activity in the HER family. BMS-599626 inhibits the kinase activity of HER1 and HER2 by competing with their ATP-binding sites, and can inhibit the downstream signaling pathway by blocking the heterodimer formation of HER1 and HER2. BMS-599626 dihydrochloride can be used to study the antitumor effects of multiple HER1 or HER2 overexpressed tumor models .
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- HY-160564
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EGFR
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Cancer
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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 .
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- HY-173511
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SARS-CoV
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Infection
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SARS-CoV-2 nsp13-IN-7 (Compound 6r) is a SARS-CoV-2 nsp13 inhibitor (IC50: 0.28 μM). SARS-CoV-2 nsp13-IN-7 interferes with the helicase function of nsp13 by binding to the 5' RNA site and ATP binding site of nsp13. SARS-CoV-2 nsp13-IN-7 can be used as a lead compound for the development of antiviral drugs targeting SARS-CoV-2 nsp13 .
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- HY-111158
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c-Met/HGFR
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Cancer
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BMS-748730 is an oral tyrosine kinase inhibitor. BMS-748730 inhibits tyrosine kinase activity by competing with the ATP binding site of the tyrosine kinase, which prevents the kinase from phosphorylating the substrate protein, thereby inhibiting signaling pathways associated with cell proliferation and tumor growth. BMS-748730 can be used in the study of certain types of cancer, including chronic myeloid leukemia (CML) .
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- HY-15463S2
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STI571-d3 hydrochloride; CGP-57148B-d3 hydrochloride
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Autophagy
Bcr-Abl
c-Kit
SARS-CoV
PDGFR
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Cancer
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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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- HY-161059
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RIP kinase
Necroptosis
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Infection
Inflammation/Immunology
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ZB-R-55 is an orally active and selective dual-mode RIPK1 inhibitor with RIPK1 IC50 values of 5.7 nM. ZB-R-55 occupies both the allosteric and ATP binding sites of RIPK1. ZB-R-55 inhibits necroptosis in cancer cells. ZB-R-55 can be used for the research of systemic inflammatory response syndrome and sepsis .
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- HY-131275
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Drug Metabolite
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Others
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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 .
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- HY-111007
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HSP
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Cancer
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CH5015765 is an orally available Hsp90 inhibitor bound to the N-terminal ATP binding site, with a dissociation constant of 3.4 nM, CH5015765 exerts antiproliferative activity against human cancer cell lines, with IC50 values of 0.46 μM for HCT116 colorectal cancer cells and 0.57 μM for NCI-N87 gastric cancer cells. CH5015765 can be used for the study of cancer .
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- HY-10261BR
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(E/Z)-BIBW 2992 (Standard)
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EGFR
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
Autophagy
Reference Standards
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Others
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(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 .
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- HY-160708
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Tie
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Cancer
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Tie2 kinase inhibitor 3 (compound 63) is a potent Tie-2 kinase inhibitor with good oral activity (IC50=30 nM). Tie2 kinase inhibitor 3 inhibits phosphorylation and signaling of Tie-2 by competing with the ATP binding site of Tie-2 kinase. This inhibition affects the stability and maturity of blood vessels, which has an impact on tumor angiogenesis. Tie2 kinase inhibitor 3 can be used to restrict tumor growth and regulate angiogenesis .
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- HY-181169
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Cyclin G-associated Kinase (GAK)
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Cancer
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GAK-IN-3 is a cyclin G-associated kinase (GAK) inhibitor with an IC50 of 207 nM and a Ki of 66 nM. GAK-IN-3 inhibits kinase activity in the nanomolar range by binding to GAK’s ATP-binding site. GAK-IN-3 acts as a cytotoxic agent that reduces viability of Ewing sarcoma cells. GAK-IN-3 can be used for the research of ewing sarcoma .
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- HY-181478
-
|
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HSP
|
Cancer
|
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Hsp90-IN-45 is a Hsp90 inhibitor. Hsp90-IN-45 competitively binds to the ATP-binding site of purified Hsp90α with a Kd of 70 nM, blocks ATP hydrolysis, and disrupts Hsp90 client signaling. Hsp90-IN-45 inhibits ATPase activity of purified Hsp90α. Hsp90-IN-45 will be radiolabeled with 76/ 77Br for use as a radiotheragnostic agent for PET imaging and Meitner-Auger electron therapy. Hsp90-IN-45 can be used for the research of cancer .
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- HY-182302
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Drug Derivative
HSP
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Cancer
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SMTIN-P01 is a TRAP1 inhibitor that is selective for cytosolic Hsp90 and accumulates in mitochondria. SMTIN-P01 binds to the ATP-binding site of TRAP1 as an ATP mimic, thereby inhibiting ATPase and foldase activities. SMTIN-P01 induces mitochondrial membrane depolarization and proteolytic degradation in cancer cells. SMTIN-P01 exhibits significant cytotoxicity, but shows extremely low toxicity to primary mouse hepatocytes, and does not interfere with SIRT3-related functions or the levels of cytosolic Hsp90 substrates. SMTIN-P01 has important application value in cancer-related research .
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- HY-183920
-
|
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CMV
p97
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Infection
|
|
LC-1310 is an antiviral agent that targets and inhibits p97, and it suppresses the in vitro replication of human cytomegalovirus (HCMV) with an EC50 value of 0.3 μM. LC-1310 targets the D2 ATP-binding site of p97, downregulates the expression of early viral proteins, thereby blocking the transcription and proliferation of early viral genes. LC-1310 can be used for research on human cytomegalovirus infection .
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- HY-182306
-
|
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VEGFR
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Cardiovascular Disease
|
|
VEGFR-2 ligand-1, Sorafenib (HY-10201) derivative, is a vascular endothelial growth factor receptor 2 (VEGFR2) ligand. VEGFR-2 ligand-1 binds to the ATP-binding pocket of VEGFR2, forms hydrophobic contacts and hydrogen bonds with key binding-site residues. VEGFR-2 ligand-1 can be used for the research angiogenesis-related pathologies .
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- HY-183627
-
|
|
PI5P4K
|
Cancer
|
|
066ATZ is a PIP4K2A/2B inhibitor with human PIP4K2A Ki 100 nM and PIP4K2B Ki 800 nM. 066ATZ binds to ATP-binding sites of PIP4K2A and PIP4K2B to block lipid kinase activity. 066ATZ can be used for the research of non-small cell lung cancer .
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- HY-182430
-
|
|
JAK
STAT
Apoptosis
|
Cancer
|
|
NVP-BVB808 is a selective and ATP-competitive JAK2 inhibitor with an IC50 of 0.35 nM. NVP-BVB808 binds to JAK2’s ATP-binding site, stabilizes JAK2’s active conformation, increases JAK2 activation loop phosphorylation, and blocks downstream kinase function. NVP-BVB808 exhibits antiproliferative and pro-apoptosis effects, suppresses constitutive STAT5a phosphorylation. NVP-BVB808 can be used for the research of cancer, such as leukemia .
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- HY-100848R
-
|
|
EGFR
Reference Standards
|
Cancer
|
|
TX1-85-1 (Standard) is the analytical standard of TX1-85-1 (HY-100848). This product is intended for research and analytical applications. 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 .
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- HY-N14094
-
|
|
JAK
Apoptosis
Autophagy
|
Cancer
|
|
Tubulosine is an alkaloid. Tubulosine can be isolated from Pogonopus tubulosus (DC.) Schumann. Tubulosine is an ATP-competitive, selective JAK3 inhibitor with an IC50 value of 9.9 nM. Tubulosine also inhibits the kinase activities of other JAK family members, the extent of inhibition is less than that of JAK3, with IC50 values of 69.5, 84.9 and 76.3 nM for JAK1, JAK2 and TYK2, respectively. Tubulosine selectively inhibits JAK3 signalling by binding to the ATP-binding site of the kinase of JAK3. Tubulosine induces apoptotic and necrotic/autophagic cell death. Tubulosine inhibits the process of peptide chain elongation by eukaryotic polysomes by, specifically preventing the elongation-factor-2-dependent step of translocation. Tubulosine exhibits anticancer activity in breast cancer cells .
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-
- HY-182037
-
|
|
DNA/RNA Synthesis
Pyruvate Kinase
|
Cancer
|
|
Multi-target kinase-IN-9 is a multi-target enzyme inhibitor with antiproliferative and antiangiogenic activities, and exhibits remarkable selectivity against hepatocellular carcinoma cells. By broadly binding to the active sites or ATP-binding regions of multiple key enzymes including DNA polymerase β, Pyruvate Kinase M2 (PKM2), Multi-target kinase-IN-9 comprehensively disrupts DNA repair and replication, glycolysis, chromatin dynamics and transcriptional programs, and blocks the self-renewal of cancer stem cells. Multi-target kinase-IN-9 induces genomic instability, lysosomal dysfunction and autophagic flux impairment, thereby triggering tumor cell death, effectively inhibiting tumor proliferation, invasion, metastasis and angiogenesis, and significantly reducing tumor volume in xenograft models. Multi-target kinase-IN-9 is applicable to hepatocellular carcinoma-related research .
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-
- HY-N17788
-
|
|
Tie
|
Cancer
|
|
6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether is a selective inhibitor of Tie2 kinase, with an IC50 value of 2.1 μM. 6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether interacts with the ATP binding site of Tie2 kinase, inhibiting kinase activity and subsequently blocking tumor angiogenesis. 6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether can be isolated from sponges of the genus Dysidea .
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-
- HY-101562R
-
|
GDC-0077 (Standard); RG6114 (Standard)
|
PI3K
Reference Standards
Apoptosis
|
Cancer
|
|
Inavolisib (Standard) is the analytical standard of Inavolisib (HY-101562). This product is intended for research and analytical applications. Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer .
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-
- HY-106005R
-
|
|
Reference Standards
Parasite
PI4K
|
Infection
|
|
MMV390048 (Standard) is the analytical standard of MMV390048 (HY-106005). This product is intended for research and analytical applications. MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=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 .
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- HY-182763
-
|
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EGFR
Raf
Caspase
Apoptosis
Bcl-2 Family
|
Cancer
|
|
EGFR/BRAFV600E-IN-7 is a dual EGFR and BRAF V600E kinase inhibitor with human IC50 values of 0.12 μM, 0.80 μM, 1.20 μM for EGFR and 0.05 μM, 0.22 μM, 0.78 μM for BRAF V600E.EGFR/BRAFV600E-IN-7 interacts with key ATP-binding site residues of EGFR and BRAF V600E, including hydrogen bonding with EGFR Met769 and BRAF V600E Cys532.EGFR/BRAFV600E-IN-7 induces apoptosis via caspase-3/8/9 activation, modulates Bax and Bcl-2 expression, scavenges free radicals, and exhibits antiproliferative activity against human cancer cell lines.EGFR/BRAFV600E-IN-7 displays drug-likeness with no PAINS/Brenk structural alerts per in silico predictions.EGFR/BRAFV600E-IN-7 can be used for the research of colon cancer, pancreatic cancer, lung cancer, breast cancer .
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-
- HY-185227
-
|
|
Ephrin Receptor
Src
Bcr-Abl
EGFR
|
Cancer
|
|
EphB4-IN-1 is a selective EphB4 tyrosine kinase inhibitor with IC50 values of 0.16-0.30 μM. EphB4-IN-1 binds to the ATP binding site of EphB4 in a DFG-in conformation, forming four stable intermolecular hydrogen bonds. EphB4-IN-1 also inhibits Src, Abl1, Lck, and EGFR kinases. EphB4-IN-1 inhibits EphB4 autophosphorylation. EphB4-IN-1 can be used for the research of cancer, such as non small cell lung cancer .
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- HY-107779R
-
|
|
Reference Standards
Raf
|
Cancer
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|
BI-882370 (Standard) is the analytical standard of BI-882370 (HY-107779). This product is intended for research and analytical applications. 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 BRAFV600E-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 .
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-
- HY-10654
-
|
|
Ephrin Receptor
|
Cancer
|
|
EphB4-IN-2 (compound 66) is a tyrosine kinase inhibitor with an IC50 value of 1.6 nM against human EphB4, and exhibits selectivity toward kinases bearing threonine gatekeeper residues. EphB4-IN-2 also has high ligand efficiency .
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-
- HY-101513R
-
|
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Eukaryotic Initiation Factor (eIF)
Reference Standards
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Neurological Disease
Cancer
|
|
eIF4A3-IN-1 (Standard) is the analytical standard of eIF4A3-IN-1 (HY-101513). This product is intended for research and analytical applications. eIF4A3-IN-1 is a selective eIF4A3 inhibitor (IC50: 0.26 μM; Kd: 0.043 μM) with cellular nonsense-mediated RNA decay (NMD) inhibitory activity. eIF4A3-IN-1 can specifically bind to the non-ATP binding site of eIF4A3. eIF4A3-IN-1 has anti-tumor and analgesic activities .
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-
- HY-171884
-
|
|
EGFR
|
Cancer
|
|
BI-8128 is a potent EGFR inhibitor, with IC50 values of 12, 6.7, 22, 10, and 3 nM against wild-type, T790M, C797S, T790M/C797S, and L858R/T790M/C797S mutant EGFR, respectively. BI-8128 significantly inhibits the proliferation of Ba/F3 and PC-9 drug-resistant mutant cells. BI-8128 is applicable for the research of non-small cell lung cancer .
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-
| Cat. No. |
Product Name |
Type |
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- HY-130777A
-
|
Adenylyl imidodiphosphate lithium hydrate
|
Biochemical Assay Reagents
|
|
AMP-PNP (Adenylyl imidodiphosphate) lithium hydrate is a non-hydrolyzable ATP analog. AMP-PNP lithium hydrate binds to ATP binding sites competely but is not hydrolyzed by enzymes, providing stable experimental conditions for studying ATP-dependent processes. AMP-PNP lithium hydrate can also be used to study enzyme activity, kinase regulation, DNA/RNA metabolism, ion channel function, and protein complex assembly .
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-
- HY-40351
-
|
|
Biochemical Assay Reagents
|
|
4-Chloro-7H-pyrrolo[2,3-d]pyrimidine is a nitrogen-containing heterocyclic organic synthesis intermediate that can be used for the synthesis of JAK and PKB/Akt inhibitors .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10280
-
|
|
ATM/ATR
|
Cancer
|
|
ATR kinase substrate peptide (ASELPASQPQPFSAKKK) is a peptide substrate for ATR protein kinase and can be used to detect ATR kinase activity .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N11784
-
|
|
Structural Classification
Terpenoids
Celastraceae
Diterpenoids
Tripterygium wilfordii Hook. f.
Plants
Source Classification
|
Apoptosis
Caspase
NF-κB
COX
IKK
|
|
Triptolidenol, a traditional Chinese medicine, is an epoxy diterpene lactone that can be isolated from Tripterygium wilfordii. Triptolidenol has anti-inflammatory and anticancer activities. Triptolidenol significantly inhibits tumor cell proliferation and migration, arrests cell cycle arrest at S phase and induces apoptosis by activating the cytochrome c/caspase cascade signaling pathway. Triptolidenol disrupts NF-κB/COX-2 pathway by inhibiting IKKβ at ATP-binding sites. Triptolidenol can be used for chronic nephritis and kidney cancer like clear cell renal cell carcinoma (ccRCC) research .
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-
-
- HY-N15301
-
|
|
Microorganisms
Ketones, Aldehydes, Acids
Source Classification
|
ROCK
Myosin
|
|
Nocarnickelamide B (Compound 2) is a linear peptide and ROCK1/2 inhibitor. Nocarnickelamide B exhibits dual inhibitory activity against ROCK1 and ROCK2 with IC50s of 14.9 μM and 21.9 μM, respectively. Nocarnickelamide B binds to the ATP-binding site. Nocarnickelamide B inhibits the activation of ROCK-regulated cytoskeletal contraction markers such as the myosin light chain. Nocarnickelamide B is potential for glaucoma reasearch .
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-
-
- HY-N14094
-
|
|
Structural Classification
Alkaloids
Other Alkaloids
Rubiaceae
Plants
Pogonopus tubulosus (A.Rich. ex DC.) K.Schum.
Source Classification
|
JAK
Apoptosis
Autophagy
|
|
Tubulosine is an alkaloid. Tubulosine can be isolated from Pogonopus tubulosus (DC.) Schumann. Tubulosine is an ATP-competitive, selective JAK3 inhibitor with an IC50 value of 9.9 nM. Tubulosine also inhibits the kinase activities of other JAK family members, the extent of inhibition is less than that of JAK3, with IC50 values of 69.5, 84.9 and 76.3 nM for JAK1, JAK2 and TYK2, respectively. Tubulosine selectively inhibits JAK3 signalling by binding to the ATP-binding site of the kinase of JAK3. Tubulosine induces apoptotic and necrotic/autophagic cell death. Tubulosine inhibits the process of peptide chain elongation by eukaryotic polysomes by, specifically preventing the elongation-factor-2-dependent step of translocation. Tubulosine exhibits anticancer activity in breast cancer cells .
|
-
-
- HY-N17788
-
|
|
Structural Classification
Monophenols
Animals
Phenols
Source Classification
|
Tie
|
|
6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether is a selective inhibitor of Tie2 kinase, with an IC50 value of 2.1 μM. 6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether interacts with the ATP binding site of Tie2 kinase, inhibiting kinase activity and subsequently blocking tumor angiogenesis. 6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether can be isolated from sponges of the genus Dysidea .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-15463S3
-
|
|
|
Imatinib- 13C,d3 (STI571- 13C,d3) is 13C 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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-
- HY-15463S2
-
|
|
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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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-
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