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CARM1-IN-1 hydrochloride

Cat. No. M13845
CARM1-IN-1 hydrochloride Structure
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Biological Activity

CARM1-IN-1 hydrochloride is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM). IC50 value: 8.6 uM Target: CRAM1 inhibitor in vitro: CARM1-IN-1 displays high and selective CARM1 inhibition, with lower or no activity against a panel of different PRMTs or HKMTs. In human LNCaP cells, CARM1-IN-1 shows a significant dose-dependent reduction of the PSA promoter activity.

*The compound is unstable in solutions, freshly prepared is recommended



Chemical Information
Molecular Weight 591.72
CAS Number 2070018-31-2
Solubility (25°C)
Storage 2-8°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Mustafa Kemal Gmş. Curr Org Synth. Green Formation of Novel Pyridinyltriazole-Salicylidene Schiff Bases

[2] No authors listed. Carteolol

[3] Mari Amino, et al. J Cardiovasc Pharmacol. Nifekalant Hydrochloride and Amiodarone Hydrochloride Result in Similar Improvements for 24-Hour Survival in Cardiopulmonary Arrest Patients: The SOS-KANTO 2012 Study

[4] P Ramalingam, et al. J Nat Sci Biol Med. Evaluation of metformin hydrochloride in Wistar rats by FTIR-ATR spectroscopy: A convenient tool in the clinical study of diabetes

[5] Ji-Tai Li, et al. Ultrason Sonochem. Synthesis of 2-(1,5-diaryl-1,4-pentadien-3-ylidene)-hydrazinecarboximidamide hydrochloride catalyzed by p-dodecylbenzenesulfonic acid in aqueous media under ultrasound irradiation

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  Catalog
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Keywords: CARM1-IN-1 hydrochloride supplier, PRMTs, inhibitors, activators


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