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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
79 Results for "
ATP-binding site
" in MedChemExpress (MCE) Product Catalog:
Products (79)
79 Results for "ATP-binding site" in MCE Product Catalog:
Cat. No.: HY-120622
CAS No.: 225521-80-2
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 .
Cat. No.: HY-W286614
CAS No.: 62001-32-5
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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 .
Cat. No.: HY-N15301
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Cat. No.: HY-163726
CAS No.: 2393787-80-7
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 .
Cat. No.: HY-155975
CAS No.: 3038119-14-8
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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) .
Cat. No.: HY-110333
CAS No.: 1781932-33-9
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 .
Cat. No.: HY-160564
CAS No.: 2767987-38-0
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 .
Cat. No.: HY-173511
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 .
Cat. No.: HY-111158
CAS No.: 910297-57-3
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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) .
Synonyms: STI571-d3 hydrochloride; CGP-57148B-d3 hydrochloride
Cat. No.: HY-161059
CAS No.: 2416593-55-8
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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 .
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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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 .
Cat. No.: HY-10261BR
CAS No.: 439081-18-2
Synonyms: (E/Z)-BIBW 2992 (Standard)
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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 .
Cat. No.: HY-160708
CAS No.: 870225-11-9
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 .
Cat. No.: HY-119831
CAS No.: 71294-60-5
Target:
NF-κB CDK PPAR Akt mTOR LXR Reactive Oxygen Species (ROS) Apoptosis Wnt Interleukin Related p38 MAPK ERK JNK
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Rohitukine is an orally active CDK9/T1 inhibitor with an IC50 of 0.3 μM. Rohitukine blocks ATP binding sites of CDK2/A and CDK9/T1, suppresses PPARγ, AKT, mTOR, C/EBPα, SREBP-2, and NF-κB signaling, and increases hepatic LXRα expression. Rohitukine induces S-phase cell cycle arrest, ROS generation, apoptosis, and exhibits anti-inflammatory activity. Rohitukine can be used for the research of leukemia, pancreatic cancer, prostate cancer, breast cancer, CNS cancer, ovarian cancer, lung cancer, dyslipidemia, inflammatory diseases, inflammatory bowel disease, and arthritis .
Cat. No.: HY-181169
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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 .
Cat. No.: HY-10654
CAS No.: 1192216-03-7
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EphB4-IN-2 is a tyrosine kinase inhibitor targeting the Eph family and Src family. EphB4-IN-2 binds to the ATP-binding site of the kinase domain of EphB4, and exhibits high affinity for tyrosine kinases with threonine as the gatekeeper residue, such as Abl, Lck and Src. EphB4-IN-2 can be used in research related to tumor-associated angiogenesis .
Cat. No.: HY-183920
CAS No.: 2322268-24-4
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 .
Cat. No.: HY-184823
CAS No.: 1417634-25-3
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CK2-IN-17 is a protein kinase CK2 inhibitor with an IC50 of 9.5 μM against human targets. CK2-IN-17 regulates the activity of protein kinase CK2 by interacting with its ATP-binding site. CK2-IN-17 can be used in studies related to protein kinase CK2-mediated pathways, such as tumors .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
