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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
2402 Results for "
integration site selection
" in MedChemExpress (MCE) Product Catalog:
Products (2402)
2402 Results for "integration site selection" in MCE Product Catalog:
213
213 Publications Verification
Cat. No.: HY-16658
CAS No.: 187389-52-2
Synonyms: Z-Val-Ala-Asp(OMe)-FMK
Z-VAD(OMe)-FMK (Z-Val-Ala-Asp(OMe)-FMK) is a cell-permeable and irreversible pan-caspase inhibitor . Z-VAD(OMe)-FMK is an ubiquitin carboxy-terminal hydrolase L1 (UCHL1) inhibitor. Z-VAD(OMe)-FMK irreversibly modifies UCHL1 by targeting the active site of UCHL1 .
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135 Cited Publications
Synonyms: STI571; CGP-57148B
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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110 Cited Publications
Research Areas:
3-TYP is an inhibitor of SIRT3 (IC50of 38 μM) and an inhibitor of Methionine Adenosyltransferase (MAT) 2 and Indoleamine 2,3-Dioxygenase (IDO). There may be many off-target sites for 3-TYP that need to be examined, such as NAD-dependent enzymes, including dehydrogenases .
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67 Cited Publications
Synonyms: VS-6063 hydrochloride; PF 04554878 hydrochloride
Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.
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55 Cited Publications
CB-5083 is a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC50 of 11 nM .
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Target:
Research Areas:
Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
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43 Cited Publications
Research Areas:
ANA-12 is a brain-penetrant, selective TrkB antagonist with IC50 values of 45.6 nM and 41.1 μM, and Kd values of 10 nM and 12 μM, for high- and low-affinity sites, respectively. ANA-12 specifically inhibits BDNF-induced TrkB receptor activation and its downstream signaling cascades by directly and non-competitively binding to the TrkB receptor, without affecting the functions of TrkA and TrkC. ANA-12 is used in research concerning neuropsychiatric disorders (such as depression and anxiety), acute and chronic pain, neuroimmune inflammation, and the mechanisms of learning and memory .
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42 Cited Publications
BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
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42 Cited Publications
BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
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41 Cited Publications
Synonyms: D-APV; D-2-Amino-5-phosphonovaleric acid
Target:
Research Areas:
D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors .
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34 Cited Publications
Synonyms: 2-ME2; NSC-659853
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27 Cited Publications
Synonyms: Mallotoxin; NSC 56346; NSC 94525
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25 Cited Publications
Synonyms: GSK 525762C; I-BET 762 besylate
Target:
Research Areas:
Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .
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Target:
Research Areas:
Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
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24 Cited Publications
Cat. No.: HY-B0789
CAS No.: 330161-87-0
SU6656 is a Src family kinases inhibitor with IC50s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.
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Lenacapavir (GS-6207) is an HIV-1 capsid inhibitor. Lenacapavir binds to the interface between capsid hexamers and CA monomers, disrupts capsid assembly and viral maturation, inhibits nuclear translocation of HIV-1 DNA, interferes with CA-mediated protein-protein interactions, reduces the formation of 2-LTR circles and pre-integration proviruses, induces aberrant capsids, and decreases the production of mature HIV-1. Lenacapavir exhibits activity against a variety of HIV-1 subtypes and clinical isolates. Lenacapavir is applicable to research related to human immunodeficiency virus type 1 (HIV-1) infection .
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Lenacapavir (GS-6207) sodium is an HIV-1 capsid inhibitor. Lenacapavir sodium binds to the interface between capsid hexamers and CA monomers, disrupts capsid assembly and viral maturation, inhibits nuclear translocation of HIV-1 DNA, interferes with CA-mediated protein-protein interactions, reduces the formation of 2-LTR circles and pre-integration proviruses, induces aberrant capsids, and decreases the production of mature HIV-1. Lenacapavir sodium exhibits activity against a variety of HIV-1 subtypes and clinical isolates. Lenacapavir sodium is applicable to research related to human immunodeficiency virus type 1 (HIV-1) infection .
21
21 Cited Publications
Cat. No.: HY-18637
CAS No.: 668467-91-2
Target:
Research Areas:
LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC50 of 25 μM.
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19 Cited Publications
Synonyms: Src Kinase Inhibitor 1; Src-l1
Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
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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
