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Results for "

PAS-B domain

" in MedChemExpress (MCE) Product Catalog:

12

Inhibitors & Agonists

4

Peptides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-108697
    PT2399
    10+ Cited Publications

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    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 .
    PT2399
  • HY-19621
    THS-044

    		HIF/HIF Prolyl-Hydroxylase Cancer
    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 .
    THS-044
  • HY-120087
    KG-548

    		MOFs HIF/HIF Prolyl-Hydroxylase Cancer
    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 .
    KG-548
  • HY-111547
    M1001

    		HIF/HIF Prolyl-Hydroxylase Cancer
    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 .
    M1001
  • HY-P10221A
    Cyclo(CKLIIF) TFA

    		HIF/HIF Prolyl-Hydroxylase Cancer
    Cyclo(CKLIIF) TFA is an inhibitor of HIF-1α and HIF-2α. The KD values of Cyclo(CKLIIF) TFA for the PAS-B domains of HIF1-α and HIF2-α are 2.6 μM and 2.2 μM, respectively. Cyclo(CKLIIF) TFA disrupts the protein-protein interaction between HIF-1α and HIF-1β. Cyclo(CKLIIF) TFA can be used in cancer research .
    Cyclo(CKLIIF) TFA
  • HY-P10426
    cyclo(CLLFVY)

    		HIF/HIF Prolyl-Hydroxylase VEGFR Cancer
    cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC50 of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers .
    cyclo(CLLFVY)
  • HY-P10222
    Cyclo(CRLLIF)

    		HIF/HIF Prolyl-Hydroxylase Cancer
    Cyclo CRLLIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 14.5 and 10.2 μM, respectively .
    Cyclo(CRLLIF)
  • HY-P10223
    Cyclo(CRVIIF)

    		HIF/HIF Prolyl-Hydroxylase Cancer
    Cyclo CRVIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 65 and 123 μM, respectively .
    Cyclo(CRVIIF)
  • HY-W470101
    HIF-2α-IN-17

    		Hsp-targeting Chimeras HIF/HIF Prolyl-Hydroxylase Apoptosis HSP Caspase Cancer
    HIF-2α-IN-17 is a selective hypoxia-inducible factor 2α (HIF2α) inhibitor that binds to the PAS-B domain of HIF2α. HIF-2α-IN-17 disrupts the interaction between HIF2α and the molecular chaperone Hsp70, leading to proteasomal degradation of HIF2α. HIF-2α-IN-17 exhibits antitumor activity and induces apoptosis in cancer cells. HIF-2α-IN-17 is applicable for research on cancers such as clear cell renal cell carcinoma .
    HIF-2α-IN-17
  • HY-183583
    HIF-2α-IN-18

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-18 is a selective HIF-2α inhibitor with a human IC50 of 8.1 nM. HIF-2α-IN-18 binds to the HIF-2α PAS-B domain, induces conformational perturbations at the HIF-2α/ARNT dimerization interface, destabilizes the HIF-2α/ARNT heterodimer, and blocks HIF-2α-mediated transcriptional activity. HIF-2α-IN-18 inhibits hypoxia-induced expression of HIF-2α target genes EPO and SERPINE1, without inhibiting HIF-1α target genes PGK1 and PDK1. HIF-2α-IN-18 can be used for the research of clear cell renal cell carcinoma, hepatocellular carcinoma[1].
    HIF-2α-IN-18
  • HY-108697R
    PT2399 (Standard)

    		Reference Standards HIF/HIF Prolyl-Hydroxylase Cancer
    PT2399 (Standard) is the analytical standard of PT2399 (HY-108697). This product is intended for research and analytical applications. 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 .
    PT2399 (Standard)
  • HY-181270
    RH01504

    		HIF/HIF Prolyl-Hydroxylase Cancer
    RH01504 is a HIF2α inhibitor with a Kd value of 5.42 nM against human HIF2α. RH01504 inhibits the growth of renal cancer cells. RH01504 can be used in research related to renal cell carcinoma .
    RH01504

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