TEPP-46 | B2164

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.

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.

B2164 | TEPP-46 DataSheet

Alternate Name/Synonyms: 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

Formulation: N/A

CAS Number: 1221186-53-3

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₁₇H₁₆N4O₂S₂

Molecular Weight: 372.5

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO (10 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent and selective PKM2 activator

MDL Number: N/A

PubChem CID: 44246499

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