TEPP-46, Catalog: B2164

Alternate Names 6-[(3-aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-5H-thieno[2’,3’:4,5]pyrrolo[2,3-d]pyridazin-5-one; CID-44246499,NCGC00186528, ML-265

Appearance White solid

CAS # 1221186-53-3

Molecular Formula C₁₇H₁₆N4O₂S₂

Molecular Weight 372.5

Purity ≥ 98% by HPLC

Solubility DMSO (10 mg/ml)

SMILES CN1C2=C(C3=C1C(=O)N(N=C3)CC4=CC(=CC=C4)N)SC(=C2)S(=O)C

InChi InChI=1S/C17H16N4O2S2/c1-20-13-7-14(25(2)23)24-16(13)12-8-19-21(17(22)15(12)20)9-10-4-3-5-11(18)6-10/h3-8H,9,18H2,1-2H3

InChi Key ZWKJWVSEDISQIS-UHFFFAOYSA-N

PubChem CID 44246499

Storage Conditions -20°C

Shipping Conditions Gel Pack

Usage For Research Use Only! Not For Use in Humans.

Handling Do not take it internally. Wear a glove and mask when handling the product. Protect from air and moisture.

TEPP-46 (ML-265) is a potent and selective PKM2 activator. TEPP-46 activates tumor-specific PKM2 (EC₅₀ = 92 nM) by binding to the dimer-dimer interface between two subunits of PKM2 and inducing tetramerization, which is the most active form of the enzyme. In mice with A549 xenograft tumors, ML-265 displays good oral bioavailability with relatively low clearance, long half-life.