Description
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.
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
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |