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505487

TEPP-46

≥98% (HPLC), solid, PKM2 activator, Calbiochem®

Synonym(s):

PKM2 Activator IV, TEPP-46, 6-((3-Aminophenyl)methyl)-4-methyl-2-methylsulfinylthieno[3,4]pyrrolo[1,3-d]pyridazin-5-one, Pyruvate Kinase M2 Activator IV, ML265, NCGC00186528, TEPP46, Pyruvate Kinase M2 Activator IV, ML265, NCGC00186528, TEPP46, 6-((3-Aminophenyl)methyl)-4-methyl-2-methylsulfinylthieno[3,4]pyrrolo[1,3-d]pyridazin-5-one

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Size/SKUAvailabilityPrice
5 mg
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$309.00

About This Item

Empirical Formula (Hill Notation):
C17H16N4O2S2
CAS Number:
1221186-53-3
Molecular Weight:
372.46
MDL number:
MFCD23160747
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light

$309.00

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Product Name

PKM2 Activator IV, TEPP-46,

assay

≥98% (HPLC)

Quality Segment

100

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

[S](=O)(C)c1[s]c2c([n](c3c2cn[n]([c]3=O)Cc4cc(ccc4)N)C)c1

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

General description

A cell-permeable thienopyrrolopyridazinone that acts as a potent allosteric PKM2 activator (AC50 = 92 nM; [PKM2] = 0.1 nM) via stoichiometric interaction (Two activator molecules per tetramer) with FBP-bound PKM2 tetramer (One FBP per monomer) in a similar manner as PKM2 Activator III (Cat. No. 504537), resulting in highly stabilized PKM2 tetramer resistant to dissociation in the presence of phosphotyrosine-containing peptide/protein or upon PKM2 K305Q mutation. Reported to exhibit good aqueous solubility (29.6 µg/mL or 79.5 µM in PBS, pH 7.4) and retard human lung carcinoma H1299 proliferation under hypoxia, but not normoxia, condition in cultures (doubling time = 50 and 35 h, respectively, with or without 30 µM TEPP-46; 1% O2) in vitro. TEPP-46 is bioavailable in mice via i.p. (Tmax = 0.5 h; Cmax = 10.854 µg/mL; AUCINF = 26.994 hr·µg/mL; 10 mg/kg) or p.o. (Tmax = 0.25 h; Cmax = 10.179 µg/mL; AUCINF = 24.350 hr·µg/mL; 10 mg/kg) administration and shown to impair H1299 tumorigenesis in mice (%tumor development/av. tumor weight = 30%/0.13 mg and 70%/2.6 mg, respectively, with or without 50 mg/kg/12 h oral dosage for 7 wks) in vivo with no apparent toxicity.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PKM2
Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Use only fresh DMSO for reconstitution.

Other Notes

Anastasiou, D., et al. 2012. Nat. Chem. Biol.8, 839.

Jiang, J.K., et al. 2010. Bioorg. Med. Chem. Lett.20, 3387.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

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PKM2 Activator IV, TEPP-46

Sigma-Aldrich

505487

PKM2 Activator IV, TEPP-46

PKM2 Activator II, DASA The PKM2 Activator II, DASA modulates the biological activity of PKM2. This small molecule/inhibitor is primarily used for Biochemicals applications.

Sigma-Aldrich

550602

PKM2 Activator II, DASA

EIF2AK3 Activator, CCT020312 The EIF2AK3 Activator, CCT020312 modulates the biological activity of EIF2AK3.

Sigma-Aldrich

324879

EIF2AK3 Activator, CCT020312

Pyruvate Kinase Activator The Pyruvate Kinase Activator controls the biological activity of Pyruvate Kinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

Sigma-Aldrich

550601

Pyruvate Kinase Activator

description

-

description

The PKM2 Activator II, DASA modulates the biological activity of PKM2. This small molecule/inhibitor is primarily used for Biochemicals applications.

description

The EIF2AK3 Activator, CCT020312 modulates the biological activity of EIF2AK3.

description

The Pyruvate Kinase Activator controls the biological activity of Pyruvate Kinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

assay

≥98% (HPLC)

assay

≥99% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

solid

form

powder

form

solid

form

powder

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

2-8°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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