Activators & Inhibitors

Ac-PAL-AMC (Legacy Tebubio ref. 282T37421). Ac-PAL-AMC is a fluorogenic substrate for the β1i/LMP2 subunit of the 20S immunoproteasome. Upon cleavage, 7-amino-4-methylcoumarin (AMC) is released, and its fluorescence can quantify the activity of the β1i/LMP2 subunit. Ac-PAL-AMC is selective for the immunoproteasome over the constitutive proteasome. AMC displays excitation/emission maxima of 351/430 nm.

Ras Inhibitory Peptide (Legacy Tebubio ref. 282T37422). Son of sevenless homolog 1 (Sos1) is a guanine nucleotide exchange factor (GEF) that directs the exchange of Ras-GDP to Ras-GTP by binding to SH3 domains of the growth factor receptor-bound protein 2 (Grb2), leading to the activation of ERK. Ras inhibitory peptide is a synthetic peptide that contains the sequence PVPPR, which corresponds to a region within human Sos1 that interacts with an SH3 domain of Grb2. It specifically blocks the interaction of the GEF with Grb2, preventing an interaction that is essential for Ras activation by receptor tyrosine kinases, including epidermal growth factor receptor.

Ras Inhibitory Peptide acetate (Legacy Tebubio ref. 282T37422L). Ras Inhibitory Peptide acetate is a peptide involved in the Ras-dependent signaling pathway that plays an important role in human cancers initiated by oncogenic receptors.

Reveromycin D (Legacy Tebubio ref. 282T37423). Reveromycin D is a bacterial metabolite originally isolated from Streptomyces. It inhibits EGF-induced mitogenic activity in Balb/MK cells and exhibits pH-dependent antifungal activity against C. albicans [MICs = 2 and >500 μg/ml at pH 3 and 7.4, respectively]. Reveromycin D also inhibits the proliferation of KB and K562 cells [IC50s = 1.6 and 1.3 μg/ml, respectively].

CAY10781 (Legacy Tebubio ref. 282T37424). CAY10781 is an inhibitor of the protein-protein interaction between neuropilin-1 (NRP-1) and VEGF-A.1It inhibits the interaction by 43% when used at a concentration of 12.5 μM. CAY10781 also inhibits VEGF-A-induced phosphorylation of VEGFR2 in catecholamine A-differentiated (CAD) cells when used at the same concentration.

FGFR4-IN-5 (Legacy Tebubio ref. 282T37425). FGFR4-IN-5, a covalent FGFR4 inhibitor, demonstrates potency and selectivity with an IC50 value of 6.5 nM. Exhibiting significant in vivo anti-tumor activity, it is applicable for research in hepatocellular carcinoma [1].

FIIN-1 (Legacy Tebubio ref. 282T37426). FIIN-1 (FGFR irreversible inhibitor-1) is an irreversible and selective FGFR inhibitor with Kd of 2.8, 6.9, 5.4, 120, 32 and 120 nM for FGFR1, FGFR2, FGFR3, FGFR4, Flt1, Flt14, respectively.FIIN-1 inhibited FGFR1, FGFR2, FGFR3, FGFR4, with IC50 of 9.2, 6.2, 11.9 and 189 nM. FIIN-1 inhibited FGFR1, FGFR2, FGFR3 and FGFR4, with IC50s of 9.2, 6.2, 11.9 and 189 nM, respectively.

(2R/S)-6-PNG (Legacy Tebubio ref. 282T37427). (2R/S)-6-PNG (6-Prenylnaringenin) is a novel natural histone deacetylase inhibitor with anticancer and antitumor activity, and it blocks T-type calcium channels to reduce neuropathic and visceral pain in mice.

TRPC6-PAM-C20 (Legacy Tebubio ref. 282T37428). TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator that induces a transient increase in intracellular Ca2+ with an EC50 of 2.37 μM in HEK cells expressing TRPC6 and enhances OAG-induced platelet aggregation.