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TAME APC inhibitor

Name: TAME
Brand: Selleck Chemicals
SKU: S2225
Availability: InStock
Rating: 5 (11 reviews)

Cat.No.S2225

Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.

Chemical Structure

Molecular Weight: 342.41

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S222501 DMSO]69 mg/mL]false]Water]69 mg/mL]false]Ethanol]3 mg/mL]false Purity: 99.96%

99.96

Related Targets	DNA/RNA Synthesis CDK Microtubule Associated Ras HSP (HSP90) PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk ROCK Myc Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 Wee1 p21 BMI-1 LIM kinase Nur77

Chemical Information, Storage & Stability

Molecular Weight	342.41	Formula	C₁₄H₂₂N₄O₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	901-47-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=CC=C(C=C1)S(=O)(=O)NC(CCCN=C(N)N)C(=O)OC

Solubility

In vitro
Batch:

DMSO : 69 mg/mL ( (201.51 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 69 mg/mL

Ethanol : 3 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.45mg/ml (10.08mM)	Taking the 1 mL working solution as an example, add 50 μL of 69 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.49mg/ml (1.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	APC ^[1]
In vitro	TAME inhibits cyclin proteolysis in mitotic Xenopus egg extract with IC50 of 12 µM. This compound at concentration of 1-200 μM arrests interphase extract treated with recombinant cyclin B1/Cdc2 complex in mitosis, with stable cyclin B1 and phosphorylated Cdc27. It at concentration of 200 μM dramaticly inhibits the ubiquitin ligase activity of the Anaphase-Promoting Complex (APC), accompanied by reduced binding of Cdh1 to APC. This chemical addition to interphase extract reduces Cdc20 association with the APC in a dose-dependent manner partly by binding directly to APC, and the contribution motif is the C-terminal isoleucine-arginine (IR) tail on APC. ^[1] It is hydrolysed by trypsin with K_m of 0.328 mM. ^[2] This compound accelerates the ATP hydrolysis process about 12-fold. ^[3] It interacts with β and γ phosphate and the adenine ring of ATP by the guanidinium group and the aromatic ring. ^[4] This chemical at concentration of 50 mM inhibits nutrient-induced germination and pressure-induced germination at 600 MPa in Bacillus subtilis. ^[5] It induces a concentration dependent contractile response on ileal strips with EC50 of 4.3 x 10³ M. ^[6]
References	https://pubmed.ncbi.nlm.nih.gov/20951947/ http://www.sciencedirect.com/science/article/pii/S0308814609012515 http://www.springerlink.com/content/1310623880656547/ https://pubmed.ncbi.nlm.nih.gov/18274689/ https://pubmed.ncbi.nlm.nih.gov/10618233/ https://pubmed.ncbi.nlm.nih.gov/9731476/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05651620	Recruiting	Calorie Restriction	Tufts University\|Pennington Biomedical Research Center\|Washington University School of Medicine\|Duke University\|National Institute on Aging (NIA)	April 6 2023	--

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