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TEPP-46

A potent and selective PKM2 activator
Catalog #: B2164

In stock

SKU-Size Size Price Qty
B2164-1 1 mg
$75.00
B2164-5 5 mg
$295.00
More Sizes Get Quote

Product Details

Alternate Name 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
Handling Protect from air and light
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

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.


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