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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
27 Results for "
PAS-B subdomain
" in MedChemExpress (MCE) Product Catalog:
Products (27)
27 Results for "PAS-B subdomain" in MCE Product Catalog:
13
13 Publications Verification
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PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo .
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SJ572403 (SJ403) is a p27 Kip1 inhibitor. SJ572403 has high specificity for specific regions within the D2 subdomain of p27-KID with a Kd value of 2.2 mM. SJ572403 can be used for the research of diseases associated with intrinsically disordered proteins (IDPs) .
Cat. No.: HY-19621
CAS No.: 62054-67-5
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THS-044 is a modulator of the formation of the HIF2α/ARNT heterodimer. THS-044 binding stabilizes the HIF2α PAS-B folded state (KD = 2 μM), for regulating HIF2 activity in endogenous and pathological settings, and does not bind to HIF1α or ARNT PAS-B. THS-044 can be used for the study of diseases related to hypoxia .
Cat. No.: HY-169996
CAS No.: 2557349-50-3
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NP3-253 is an orally active and brain-penetranted NLRP3 inflammasome inhibitor. NP3-253 functions as a molecular glue that prevents NACHT-subdomain rearrangements, locking NLRP3 in an inactive conformation. NP3-253 inhibits production of pro-inflammatory cytokines IL-1β and IL-18. NP3-253 can be used for the research of inflammation and neurological disease, suah as peritonitis .
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KG-548 is an ARNT/TACC3 disruptor and a HIF-1α inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as HIF-β .
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M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic kidney disease research .
ADH-6 TFA is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 TFA targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 TFA has the potential for the research of cancer diseases .
Cat. No.: HY-P10426
CAS No.: 1446322-73-1
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Cat. No.: HY-P10221A
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Cat. No.: HY-168992
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UNC6535 is a covalent ligand targeting the SETDB1 triple Tudor domain (3TD) with negative allosteric modulator properties, with an IC50 of 3.4 μM and a Kd of 4.2 μM. UNC6535 inhibits the methyltransferase activity of recombinant SETDB1 protein lacking the 3TD domain. UNC6535 reversibly binds to the aromatic cages of both TD2 and TD3 subdomains of SETDB1 3TD simultaneously, displacing the endogenous H3K9Me2K14Ac histone tail ligand. UNC6535 can be used in research on cancer and neurodegenerative diseases .
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-W028350
CAS No.: 40106-12-5
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NSC727447 is a vinyl urea-based allosteric inhibitor of HIV reverse transcriptase-associated RNase H with IC50 values of 2.0 μM and 2.5 μM against HIV-1 and HIV-2 RNase H, respectively, and IC50 values of 100 μM and 10.6 μM against Escherichia coli and human RNase H, respectively. NSC727447 exerts allosteric inhibitory effects mainly by interacting with the region adjacent to α-helix I in the thumb subdomain of the p51 subunit of HIV-1 reverse transcriptase. Cys280, Lys281 and the RNase H primer grip region are involved in its action, and it may inhibit the catalytic activity of RNase H by altering the positioning of nucleic acid substrates or the geometry of the RNase H active site. NSC727447 can be used in studies related to HIV infection, the function of HIV reverse transcriptase RNase H, and allosteric inhibition mechanisms .
Cat. No.: HY-P10222
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Cat. No.: HY-125864A
CAS No.: 9001-32-5
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Canine Fibrinogen is a natural fibrinogen derived from canine plasma. Canine Fibrinogen specifically binds to the host SpsL, but shows weak binding affinity to fibrinogen from other mammals including humans. Canine Fibrinogen binds to the N2N3 subdomain of SpsL via the "anchor-lock-latch" model, and interacts with multiple sites in its α-chain C domain. The binding of Canine Fibrinogen to SpsL promotes bacterial aggregation, biofilm formation, and enhances bacterial resistance to neutrophil phagocytosis. Canine Fibrinogen can be used in studies related to canine skin infections .
Cat. No.: HY-W012248
CAS No.: 349-58-6
KG-655 is a ligand that specifically binds to the ARNT PAS-B domain. KG-655 binds to the internal cavity of ARNT PAS-B to restrict its variable folded conformation, disrupts the interaction between ARNT PAS-B and the transcriptional coactivator TACC3, and promotes the homodimerization of ARNT PAS-B. KG-655 is widely applicable to cancer-related research .
Cat. No.: HY-P5379
CAS No.: 128578-18-7
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Cat. No.: HY-145785
CAS No.: 2227429-65-2
ADH-6 is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 has the potential for the research of cancer diseases[1].
Cat. No.: HY-P10223
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Cat. No.: HY-177710
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MEDI4276 is a biparatopic tetravalent antibody targeting two nonoverlapping epitopes in subdomains 2 and 4 of the HER2 ecto-domain. MEDI4276 is composed of MEDI4276 Antibody (HY-P991238) and a cytotoxic payload AZ1508 (HY-128962) linked through site-specific coupling. MEDI4276 exhibits antitumor activity .
Cat. No.: HY-111547R
CAS No.: 874590-32-6
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M1001 (Standard) is the analytical standard of M1001 (HY-111547). This product is intended for research and analytical applications. M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic Kidney disease 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
