TEPP-46 (ML265) - Moligand™, 10mM in DMSO , Activator of pyruvate kinase M1/2, CAS No.1221186-53-3, Activator of pyruvate kinase M1/2

CAS: 1221186-53-3 Cat. No.: T408345 Formula: C₁₇H₁₆N₄O₂S₂ Molecular Weight: 372.5

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

CID-44246499, NCGC00186528 | 5H-​Thieno[2',​3':4,​5]​pyrrolo[2,​3-​d]​pyridazin-​5-​one, 6-​[(3-​aminophenyl)​methyl]​-​4,​6-​dihydro-​4-​methyl-​2-​(methylsulfinyl)​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

TEPP-46 (ML265) TEPP-46 (ML265, CID-44246499, NCGC00186528) is a potent activator of PKM2 in both biochemical (AC50 = 92 nM) and cell-based assays with high selectivity over PKM1, PKR and PKL.
In vitro

ML265 potently activates PKM2 in vitro with an AC50 = 92 nM and shows a high degree of selectivity over the other 3 pyruvate kinase isoforms. ML265 binds at the dimer-dimer interface of the PKM2 homotetramer. It is capable of activating PKM2 in cell lysate of pervanadate treated cells, which is a condition known to inhibit PKM2 activity through accumulation of phosphotyrosine peptides. ML265 significantly increased the doubling time of H1299 cells under hypoxic conditions, but interestingly showed no effect under normoxia.

In vivo

ML265 gave superior plasma concentrations that persisted at higher levels over the 24 hour study. ML265 also displayed good oral bioavailability, low clearance, a long half-life and good volume of distrubtion. The 7-week mouse xenograft model (H1299 mouse xenograft) showed that the activation of PKM2 with ML265 was able to significantly reduce tumor size and occurrence without showing signs of acute toxicity. .
Cell Data

cell lines：CHO-K1 cells

Concentrations：50 μM

Incubation Time：1 h

Powder Purity:≥98%

Specifications

Synonyms

CID-44246499, NCGC00186528 | 5H-​Thieno[2',​3':4,​5]​pyrrolo[2,​3-​d]​pyridazin-​5-​one, 6-​[(3-​aminophenyl)​methyl]​-​4,​6-​dihydro-​4-​methyl-​2-​(methylsulfinyl)​-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

TEPP-46 (ML265, CID-44246499, NCGC00186528) is a potent activator of PKM2 in both biochemical (AC50 = 92 nM) and cell-based assays with high selectivity over PKM1, PKR and PKL.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ACTIVATOR

Mechanism of action

Activator of pyruvate kinase M1/2

Names and Identifiers

• Isomeric SMILES: CN1C2=C(C3=C1C(=O)N(N=C3)CC4=CC(=CC=C4)N)SC(=C2)S(=O)C
• Molecular Weight: 372.5
• Reaxy-Rn: 20138466
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20138466&ln=

Associated Targets(Human)

PKM Tchem Pyruvate kinase PKM (0 Activities)

Discover Target: PKM

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro Ethanol: mg/mL
• Refractive Index: n20D1.81 (Predicted)
• Boil Point(°C): ~711.6° C at 760 mmHg (Predicted)

Frequently Asked Questions

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1221186-53-3, the molecular formula is C17H16N4O2S2, and the molecular weight is 372.5 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.