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Chemical Structure| 42924-53-8 Chemical Structure| 42924-53-8
Chemical Structure| 42924-53-8
Product Citations

Product Citations

Wegner, Scott A ; Kim, Hahn ; Avalos, José L ;

Abstract: Lactate transport plays a crucial role in the metabolism, microenvironment, and survival of cancer cells. However, current drugs targeting either MCT1 or MCT4, which traditionally mediate lactate import or efflux respectively, show limited efficacy beyond in vitro models. This limitation partly arises from the existence of both isoforms in certain tumors, however existing high-affinity MCT1/4 inhibitors are years away from human testing. Therefore, we conducted an optogenetic drug screen in Saccharomyces cerevisiae on a subset of the FDA-approved drug library to identify existing scaffolds that could be repurposed as monocarboxylate transporter (MCT) inhibitors. Our findings show that several existing drug classes inhibit MCT1 activity, including non-steroidal estrogens, non-steroidal anti-inflammatory drugs (NSAIDs), and natural products (in total representing approximately 1% of the total library, 78 out of 6400), with a moderate affinity (IC50 1.8–21 μM). Given the well-tolerated nature of NSAIDs, and their known anticancer properties associated with COX inhibition, we chose to further investigate their MCT1 inhibition profile. The majority of NSAIDs in our screen cluster into a single large structural grouping. Moreover, this group is predominantly comprised of FDA-approved NSAIDs, with seven exhibiting moderate MCT1 inhibition. Since these molecules form a distinct structural cluster with known NSAID MCT4 inhibitors, such as diclofenac, ketoprofen, and indomethacin, we hypothesize that these newly identified inhibitors may also inhibit both transporters. Consequently, NSAIDs as a class, and piroxicam specifically (IC50 4.4 μM), demonstrate MCT1 inhibition at theoretically relevant human dosages, suggesting immediate potential for standalone MCT inhibition or combined anticancer therapy.

Alternative Products

Product Details of Nabumetone

CAS No. :42924-53-8
Formula : C15H16O2
M.W : 228.29
SMILES Code : CC(CCC1=CC=C2C=C(OC)C=CC2=C1)=O
Synonyms :
BRL14777
MDL No. :MFCD00079518
InChI Key :BLXXJMDCKKHMKV-UHFFFAOYSA-N
Pubchem ID :4409

Safety of Nabumetone

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • COX

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01638962 Osteoarthritis, Knee Not Applicable Completed - Denmark ... More >> University of Southern Denmark Odense, Region Syddanmark, Denmark, 5230 Less <<
NCT01761864 Study Focus: Prescribing of Dr... More >>ugs Less << Not Applicable Unknown January 2016 Belgium ... More >> University of Antwerp Wilrijk, Belgium, 2610 Less <<
NCT00363532 Migraine Without Aura Not Applicable Completed - Denmark ... More >> Danish Headache Center, Neurological Dep. Glostrup hospital Glostrup, Denmark, 2770 Less <<
NCT02865369 - Not yet recruiting December 2022 Korea, Republic of ... More >> Soonchunhyang University Cheonan Hospital Recruiting Cheonan, Chungcheongnam-do, Korea, Republic of, 31151 Contact: SaeHwan Lee, Professor          Principal Investigator: SaeHwan Lee, Professor          Soon Chun Hyang University Bucheon Hospital Recruiting Bucheon, Gyeonggi do, Korea, Republic of, 14584 Contact: Sang Gyune Kim, Professor    82-32-621-5079    mcnulty@schmc.ac.kr    Principal Investigator: Sang Gyune Kim          Korea University Ansan Hospital Recruiting Ansan, Gyeonggi-do, Korea, Republic of, 15355 Contact: Young Kul Jung, Professor          Principal Investigator: Young Kul Jung, Professor          Inha University Hospital Recruiting Jung-gu, Incheon, Korea, Republic of, 22332 Contact: Jin-Woo Lee, Professor          Principal Investigator: Jin-Woo Lee, Professor          Gachon University Gil Medical Center Recruiting Incheon, Korea, Republic of, 21565 Contact: Oh Sang Kwon, Professor          Principal Investigator: Oh Sang Kwon, Professor          Severance hospital Recruiting Seoul, Korea, Republic of, 03722 Contact: Jun Yong Park, Professor          Principal Investigator: Jun Yong Park, Professor          Soonchunhyang University Hospital Recruiting Seoul, Korea, Republic of, 04401 Contact: Jae Young Jang, Professor          Principal Investigator: Jae Young Jang, Professor          Hanyang university hospital Recruiting Seoul, Korea, Republic of, 04763 Contact: Dae Won Jun, Professor          Principal Investigator: Dae Won Jun, Professor          Ewha Womans University Mokdong Hospital Recruiting Seoul, Korea, Republic of, 07985 Contact: Tae Hun Kim, Professor          Principal Investigator: Tae Hun Kim, Professor          Wonju severance christian hospital Recruiting Wonju, Korea, Republic of, 26426 Contact: Moon young Kim, Professor          Principal Investigator: Moon young Kim, Professor Less <<
NCT00864968 Healthy Phase 1 Completed - United States, North Carolina ... More >> AAIPharma Inc., AAI Clinic Morrisville, North Carolina, United States, 27560 Less <<
NCT02049606 Osteoarthritis of the Knee Phase 4 Completed - Korea, Republic of ... More >> Asan Medical Center Seoul, Korea, Republic of Chung-Ang University Hospital Seoul, Korea, Republic of Inje University Seoul Paik Hospital Seoul, Korea, Republic of Seoul National University Hospital Seoul, Korea, Republic of SMG-SNU Boramae Medical Center Seoul, Korea, Republic of The Catholic University of Korea, Seoul ST. Mary's Hospital Seoul, Korea, Republic of Less <<
NCT01164813 Healthy Phase 1 Completed - India ... More >> Bioserve Clinical Research Pvt. Ltd. Hyderabad, Andhra Pradesh, India, 500037 Less <<
NCT01164826 Healthy Phase 1 Completed - India ... More >> Bioserve Clinical Research Pvt. Ltd. Hyderabad, Andhra Pradesh, India, 500037 Less <<
NCT00864604 Healthy Phase 1 Completed - United States, North Carolina ... More >> AAIPharma Inc., AAI Clinic Morrisville, North Carolina, United States, 27560 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.38mL

0.88mL

0.44mL

21.90mL

4.38mL

2.19mL

43.80mL

8.76mL

4.38mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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