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Chemical Structure| 1613710-01-2 Chemical Structure| 1613710-01-2

Structure of ARN-3236
CAS No.: 1613710-01-2

Chemical Structure| 1613710-01-2

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ARN-3236 is a selective and orally bioavailable inhibitor of salt-inducible kinase 2 (SIK2), with IC50 values of <1 nM for SIK2, 21.63 nM for SIK1, and 6.63 nM for SIK3. It exhibits antitumor activity.

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Product Details of ARN-3236

CAS No. :1613710-01-2
Formula : C19H16N2O2S
M.W : 336.41
SMILES Code : COC1=CC=C(C2=CNC3=NC=CC(C4=CSC=C4)=C32)C(OC)=C1
MDL No. :MFCD31813721
InChI Key :WEHOIIGXTMKVRG-UHFFFAOYSA-N
Pubchem ID :74766530

Safety of ARN-3236

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

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HCT8 5 μM 24 hours To evaluate the effect of ARN-3236 on cell survival after radiation, results showed that ARN-3236 significantly enhanced cell sensitivity to radiation. PMC11774237
HCT116 5 μM 24 hours To evaluate the effect of ARN-3236 on cell survival after radiation, results showed that ARN-3236 significantly enhanced cell sensitivity to radiation. PMC11774237
SIK2-overexpressed HFLs (HFLs-SIK2) 0.5 μM 30 minutes ARN-3236 inhibited SIK2 activity, reduced CRTC2 phosphorylation, and suppressed fibroblast differentiation and ECM expression. PMC9004037
A2780 0.93 μM (IC50) 48 hours ARN-3236 inhibited A2780 cell growth with an IC50 of 0.93 μM and increased nuclear-centrosome distance. PMC5436602
SKOv3 1.23 μM (IC50) 72 hours ARN-3236 inhibited SKOv3 cell growth with an IC50 of 1.23 μM. PMC5436602
OVCAR8 1.56 μM (IC50) 96 hours ARN-3236 enhanced paclitaxel sensitivity in OVCAR8 cells. PMC5436602
OC316 1.63 μM (IC50) 96 hours ARN-3236 enhanced paclitaxel sensitivity in OC316 cells. PMC5436602

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Subcutaneous xenograft model Oral 40 mg/kg Once daily for 7 days To evaluate the effect of ARN-3236 on radiotherapy efficacy, results showed that ARN-3236 significantly enhanced the inhibitory effect of radiotherapy. PMC11774237
Nude mice SKOv3ip and OVCAR8 xenograft models Oral 60 mg/kg Once daily for 7 days ARN-3236 enhanced the antitumor effect of paclitaxel in SKOv3ip and OVCAR8 xenograft models. PMC5436602
C57BL/6J mice Chronic social defeat stress (CSDS) and chronic unpredictable mild stress (CUMS) models of depression Intraperitoneal injection 1, 3, 10, 30, 60 mg/kg Daily for 2 weeks ARN-3236 exhibited significant antidepressant-like effects in both CSDS and CUMS models, accompanied by fully preventing stress-enhanced SIK2 expression and cytoplasmic translocation of CRTC1 in the hippocampus. ARN-3236 treatment also completely reversed the down-regulating effects of CSDS and CUMS on the hippocampal BDNF system and neurogenesis. PMC7840484
BALB/c mice Bleomycin-induced pulmonary fibrosis model Intraperitoneal injection 10 mg/kg and 30 mg/kg Once daily for 14 or 28 days ARN-3236 dose-dependently attenuated bleomycin-induced pulmonary fibrosis, reducing collagen deposition and α-SMA expression. PMC9004037

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.97mL

0.59mL

0.30mL

14.86mL

2.97mL

1.49mL

29.73mL

5.95mL

2.97mL

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
 

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