GT-002

GT-002 binds with high affinity to the GABA_A receptor benzodiazepine site (K_i = 0.57 nM, IC₅₀ = 0.68 nM), shows minimal off-target binding to the dopamine transporter, and acts as a partial positive allosteric modulator inducing only 10-20% of the Cl⁻ current activation of diazepam^[1].
GT-002 specifically binds the tumor-associated protein/carbohydrate combined epitope on LYPD3 in ELISA, with no binding to non-glycosylated LYPD3 or the target carbohydrate on unrelated proteins^[2].
GT-002 (10^-3-10⁴ ng/mL; 1.5 h) specifically binds to a combined TF-LYPD3 glycopeptide epitope, with an EC₅₀ of 5.5 ng/mL for TF-carrying recombinant LYPD3, and does not bind non-glycosylated LYPD3, Tn-carrying LYPD3, sialylated LYPD3, or irrelevant TF-carrying glycoproteins^[3].
GT-002 (10 μg/mL; 30 min at 4°C) binds specifically to cell surface-expressed TF-glycosylated LYPD3 on LYPD3-F9 recombinant cells and neuraminidase-treated LYPD3-positive CaOV-3 and ZR-75-1 tumor cells, but not to non-glycosylated LYPD3, LYPD3-negative tumor cells, or untreated LYPD3-positive tumor cells^[3].
GT-002 (10 μg/mL; overnight/incubation) binds to TF-glycosylated LYPD3 in a range of human SCC tumor tissues, and shows highly restricted binding to normal human tissues (only skin epidermis), with normal tissue binding re-established by neuraminidase treatment due to sialic acid masking of its epitope^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.