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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
37 Results for "
ATP binding domain
" in MedChemExpress (MCE) Product Catalog:
Products (37)
37 Results for "ATP binding domain" in MCE Product Catalog:
51
51 Publications Verification
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CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation .
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11 Cited Publications
Cat. No.: HY-17537
CAS No.: 1216665-49-4
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain .
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BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys 496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
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Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor .
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2 Cited Publications
AMP-PCP disodium is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP disodium binding favors the formation of the active homodimer of Hsp90 .
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2 Cited Publications
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NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate .
Cat. No.: HY-173432
CAS No.: 3111845-07-6
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LIBX-A401 is a selective long-chain acyl-CoA synthetase 4 (ACSL4) inhibitor with a human IC50 values of 0.38 μM and a Kd of 0.72 μM. LIBX-A401 binds to ACSL4 in an ATP-dependent manner, stabilizes the C-terminal domain, alters the fatty acid gate region, and interacts with residues A329 and Q302 within the fatty acid binding site. LIBX-A401 exhibits anti-ferroptosis properties in cells. LIBX-A401 can be used for the researches of cancer and parkinson's disease .
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PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain .
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NR162 is a selective CASK (Ca 2+/calmodulin-dependent Ser/Thr kinase) inhibitor with an IC50 of 80 nM and a Kd of 22 nM. NR162 shows about 50-fold selectivity for CASK than TYRO3. NR162 targets the unique GFG motif of CASK and has excellent shape complementarity to the CASK ATP binding pocket. NR162 can be used for the research of neurological diseases .
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R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC50 of 38 nM for human LIMK1 .
Cat. No.: HY-175278
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BAL-1516 is an orally active NLRP3 inhibitor with human NLRP3 Kd of 14.2 nM, mouse NLRP3 Kd of 200 nM, and blood-brain barrier penetration.BAL-1516 binds to a surface groove of the NLRP3 nucleotide-binding domain, contacts FISNA and WHD subdomains, forms three hydrogen bonds to the peripheral β-strand of the triple-ATPase, and does not alter NLRP3 ATP-hydrolysis activity.BAL-1516 shows specificity for NLRP3 over other NOD-like receptors, directly binds mouse NLRP3, and inhibits inflammasome formation in monocytes and microglia .
Cat. No.: HY-160519
CAS No.: 955918-74-8
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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 .
Cat. No.: HY-122184
CAS No.: 34387-64-9
PET-16 is a selective HSP70 inhibitor that binds to an allosteric pocket of the substrate-binding domain. PET-16 inhibits the ability of HSP70 to cycle between ATP-bound and ADP-bound states. PET-16 induces apoptosis in multiple myeloma .
Cat. No.: HY-145425
CAS No.: 2771006-54-1
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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 .
Cat. No.: HY-N2452
CAS No.: 956103-79-0
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Cat. No.: HY-122735
CAS No.: 690216-38-7
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Inh2-B1 is a Ser/Thr protein kinase (STK1) inhibitor. Inh2-B1 specifically inhibits STK1 activity by directly binding to its ATP-binding catalytic domain. Inh2-B1 down-regulates cell wall hydrolase genes and disrupts the biofilm formation of Methicillin-resistant Staphylococcus aureus (MRSA) clearly .
Cat. No.: HY-P11053
CAS No.: 1140483-31-3
Cat. No.: HY-W107722
CAS No.: 838816-57-2
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IN04 is a inhibitor of leucine-rich repeat kinase 1 (LRRK1). IN04 can completely block the binding of ATP to the human LRRK1 kinase domain, thereby inhibiting the kinase activity of LRRK1. IN04 can significantly impair the bone resorption ability of osteoclasts, with an IC50 value of 5.72 μM. IN04 can be used for the study of osteoporosis .
Cat. No.: HY-177936
CAS No.: 951950-33-7
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NAE-IN-3 (compound 1) is a potent, selective and non-covalent competitive NEDD8-activating enzyme (NAE) inhibitor (IC50 = 0.8 μM). NAE-IN-3 inhibits NAE by blocking the ATP-binding domain. NAE-IN-3 exhibits selectivity over analogous E1 enzymes UAE and SAE. NAE-IN-3 can be used for cancer research .
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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
