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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
121 Results for "
ATP pocket
" in MedChemExpress (MCE) Product Catalog:
Products (121)
121 Results for "ATP pocket" in MCE Product Catalog:
149
149 Publications Verification
SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits . SB202190 induces autophagy .
149
149 Publications Verification
SB 202190 hydrochloride is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 hydrochloride binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 hydrochloride has anti-cancer activity . SB202190 hydrochloride induces autophagy .
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Target:
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Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL). Acalabrutinib can be used for CLL research . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
33
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Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
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16 Cited Publications
Synonyms: 5,7-Dihydroxy-4'-methoxyflavone
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12 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 .
3
Category:
Quinones Plant Other Diseases Other Families Extract Disease Research Fields Naphthalene Quinones Alkanna cappadocica Extract
Target:
2
2 Cited Publications
INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells .
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1
1 Cited Publications
Synonyms: PLB-1001; CBT-101; Vebreltinib
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Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily .
1
1
1 Cited Publications
G907 is a selective antagonist of ATP-binding cassette (ABC) transporter MsbA with anti-microbial activity. G907 inhibits E. coli MsbA with an IC50 value of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket .
1
1 Cited Publications
Target:
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UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor, binds in the MerTK ATP pocket, with an IC50 of 4.4 nM, more selective over Axl, Tyro3 and Flt3. UNC2541 inhibits phosphorylated MerTK (pMerTK; EC50, 510 nM). UNC2541 abolishes the analgesic and anti-inflammatory effects of ozone in vivo and in vitro .
1
1 Cited Publications
Cat. No.: HY-175328
Target:
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LIBX-A403 is a potent, selective and reversible ACSL4 inhibitor with a human IC50 of 0.049 μM and a Kd of 0.29 μM. LIBX-A403 binds in the ACSL4 fatty acid pocket in an ATP-dependent manner. LIBX-A403 prevents cell ferroptosis. LIBX-A403 can be used for the researches of cancer and parkinson's disease .
1
1 Cited Publications
Cat. No.: HY-164145
CAS No.: 3034216-44-6
Target:
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CDD-1653 is a potent and selective BMPR2 inhibitor with an IC50 of 2.8 nM. CDD-1653 inhibits the catalytic activity of BMPR2 by competitively binding to its ATP pocket, specifically blocking BMP-induced downstream signaling (particularly inhibiting SMAD1/5 phosphorylation), thereby suppressing the expression of related genes. CDD-1653 can be used for research on cancer, bone diseases, and vascular and endothelial dysfunction .
1
1 Cited Publications
Cat. No.: HY-155583
Purity: 98.08%
Target:
Research Areas:
RNase L-IN-1 is a RNase L inhibitor with an IC50 of 15.9 μM. RNase L-IN-1 binds to the ATP-binding pocket of RNase L, and inhibits ribosomal RNA cleavage. RNase L-IN-1 can be used for the research of RNase L-associated cellular processes .
1
1 Cited Publications
Cat. No.: HY-155583A
Purity: 99.56%
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RNase L-IN-1 trihydrochloride is a RNase L inhibitor with an IC50 of 15.9 μM. RNase L-IN-1 trihydrochloride binds to the ATP-binding pocket of RNase L, and inhibits ribosomal RNA cleavage. RNase L-IN-1 trihydrochloride can be used for the research of RNase L-associated cellular processes .
Synonyms: ART0380
Research Areas:
ART0380 is a potent, selective and orally active ATR kinase inhibitor. ART0380 potently inhibits human ATR-ATRIP complex with an IC50 of 51.7 nM. ART0380 binds the ATP pocket of the ATR-ATRIP complex, blocks ATR-dependent Chk1 serine 345 phosphorylation, and induces cell cycle disorder and DNA damage. ART0380 demonstrates potent and selective antitumor activity in preclinical models with varying types of ataxia-telangiectasia mutated (ATM) gene aberrancy. ART0380 can be used for the research of cancer, such as colorectal cancer and prostate cancer .
Cat. No.: HY-160196
CAS No.: 2803470-63-3
Synonyms: GCN2 modulator-1
Research Areas:
HC-7366 (GCN2 modulator-1) is an orally effective GCN2 activator. HC-7366 can effectively compete and occupy the ATP binding pocket of GCN2, with its IC50 being 72 nM. This binding triggers the conformational activation of GCN2, leading to the upregulation of downstream signals (such as ATF4, ASNS) in the integrated stress response (ISR) pathway, ultimately exerting anti-tumor effects. HC-7366 also has inhibitory activity against ZAK, with its IC50 being 47 nM. HC-7366 can be used for research on fibrosarcoma and acute myeloid leukemia .
BRITE-338733 is an inhibitor of E. coli RecA ATPase activity (IC50: 4.7 μM). BRITE-338733 also inhibits the ATP hydrolysis activity of RSC chromatin remodeling enzyme by binding to its ATP-binding pocket and DNA (IC50: 0.316 μM). BRITE-338733 exhibits cytotoxicity against MCF-7 and MDA-MB-231 breast cancer cells. BRITE-338733 can be used in studies on antibacterial adjuvants and anticancer 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
