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WT mice

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9

Inhibitors & Agonists

1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-121845
    4-Br-Bnlm

    		HSP Metabolic Disease
    4-Br-Bnlm is a selective inhibitor of glucose-regulated protein 94 (Grp94) with an EC50 value of 0.96 µM. 4-Br-Bnlm reduces the levels of mutant myocilin proteins as well as wild-type myocilin misfold in cells. 4-Br-Bnlm promotes the clearance of toxic formsof myocilin and reduces myocilin toxicity .
    4-Br-Bnlm
  • HY-158991
    I1421

    		CFTR Inflammation/Immunology
    I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) with an EC50 of 64 nM for WT CFTR currents. I1421 also allosterically activates multiple mutants causing cystic fibrosis (CF) with good in vivo potency, with an oral bioavailability of 60% in mice corresponding to a half-life of 75 min. I1421 synergizes with Elexacaftor (HY-111772) to enhance CFTR currents .
    I1421
  • HY-139178
    KVA-D-88

    		Phosphodiesterase (PDE) Neurological Disease
    KVA-D-88 is a blood-brain barrier-permeable PDE4 inhibitor with IC50 values of 140 and 880 nM for PDE4B and PDE4D, respectively. KVA-D-88 has the ability to inhibit cocaine-induced hyperlocomotor activity and sensitization. KVA-D-88 selectively inhibits PDE4B and reduces cAMP degradation, thereby modulating neuroadaptive responses. KVA-D-88 can be used in the study of cocaine addiction .
    KVA-D-88
  • HY-118574
    UBP141

    		iGluR Neurological Disease
    UBP141 is a GluN2C/2D (NR2C/2D)-preferring receptor antagonist, with Kds of 2.8, 4.2, 14.2, and 19.3 μM for NMDA receptor subtypes: GluN2C, 2D, 2A, and 2B, respectively. UBP141 can induce potent motor impairment in WT mice .
    UBP141
  • HY-151155
    ALK-IN-23

    		Anaplastic lymphoma kinase (ALK) Cancer
    ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALK WT, ALK L1196M and ALK G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity .
    ALK-IN-23
  • HY-144655
    IP2

    		Phosphatase Cancer
    IP2 is an immunomodulatory agent. IP2 increases PTP (Pioneer Translation Product)-derived antigen presentation in cancer cells. IP2 shows non-cytotoxic for cancer cells. IP2 induces tumor growth defects in mouse .
    IP2
  • HY-159159
    MS-II-124

    		NOD-like Receptor (NLR) Inflammation/Immunology
    MS-II-124 is an effective and selective NLRP3 inhibitor (IC50=0.12 μM) with anti-inflammatory and immunomodulatory activities, which can be used in the research of acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) .
    MS-II-124
  • HY-146019
    HIV-1 inhibitor-24

    		HIV Infection
    HIV-1 inhibitor-24 (compound S-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 9.5 nM. HIV-1 inhibitor-24 has high antiretroviral activity against WT HIV-1 with an EC50 of 1.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 9.07 μM in MT-4 cells. HIV-1 inhibitor-24 is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety .
    HIV-1 inhibitor-24
  • HY-149401
    EGFR-IN-82

    		EGFR Cancer
    EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFR WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
    EGFR-IN-82

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