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K1053

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4

Inhibitors & Agonists

1

Inhibitory Antibodies

1

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111419
    DSP-1053

    		Serotonin Transporter 5-HT Receptor Neurological Disease
    DSP-1053, a benzylpiperidine derivative, is a potent Serotonin Transporter (SERT) inhibitor with a Ki of 1.02 nM. DSP-1053 shows partial 5-HT1A receptor agonistic activity with a Ki of 5.05 nM. DSP-1053 has antidepressant activity .
    DSP-1053
  • HY-P991063
    GEN-1053

    BNT-313; Tixestobart

    		 TNF Receptor Inflammation/Immunology Cancer
    GEN-1053 (BNT-313) is a fully human IgG1 antibody that targets CD27. GEN-1053 binds to CD27 and forms a hexamer upon binding. The isotype control for GEN-1053 can refer to Human IgG1 lambda1, Isotype Control (HY-P99992) .
    GEN-1053
  • HY-117087
    K103

    		Phosphatase PANoptosis Cancer
    K103 is an inhibitor discovered from the screen that is an analog of the serotonin antagonist benzazocine. K103 exhibited inhibition of SHIP homologues, labelling it a pan-SHIP1/2 inhibitor, but the molecule had no effect on another 5' inositol phosphatase, OCRL. In line with the "two PIPs hypothesis", the molecule exhibited significant anti-tumour effects against a variety of cell lines, particularly breast cancer cells. Additional studies with K103 revealed that inhibition of SHIP1/2 in multiple myeloma cells resulted in G2/M cell cycle arrest followed by extensive apoptosis via activation of the caspase cascade. K103 fits the commonly used small molecule agent property profile, but while this work was being conducted, it was discovered that K103 caused psychoactive effects in mice, which limited the utility of the molecule in vivo. Therefore, certain synthetic studies were conducted on this tryptamine to identify the features that needed to be present in the molecule to maintain pan-SHIP1/2 inhibition in order to design an inhibitor with favourable pharmacodynamic properties and an improved side effect profile.
    K103
  • HY-111419A
    DSP-1053 benzenesulfonate

    		Serotonin Transporter 5-HT Receptor Neurological Disease
    DSP-1053, a benzylpiperidine derivative, is a potent serotonin transporter (SERT) inhibitor with a Ki of 1.02 nM. DSP-1053 shows partial 5-HT1A receptor agonistic activity with a Ki of 5.05 nM. DSP-1053 has antidepressant activity .
    DSP-1053 benzenesulfonate

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