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ARN-3236

Catalog No. T5993 CAS 1613710-01-2

ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), (SIK2, SIK1 and SIK3 with IC50s of <1 nM, 21.63 nM and 6.63 nM respectively). ARN-3236 Has anti-cancer activity.

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ARN-3236, CAS 1613710-01-2

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), (SIK2, SIK1 and SIK3 with IC50s of <1 nM, 21.63 nM and 6.63 nM respectively). ARN-3236 Has anti-cancer activity.
Targets&IC50	SIK3:6.63.nM, SIK2:<1 nM , SIK1:21.63 nM
In vitro	Salt-inducible kinase 2 (SIK2) is overexpressed in approximately 30% of high-grade serous ovarian cancers.?ARN-3236 inhibited the growth of 10 ovarian cancer cell lines at an IC50 of 0.8 to 2.6 μmol/L, where the IC50 of ARN-3236 was inversely correlated with endogenous SIK2 expression (Pearson r = -0.642, P = 0.03).?ARN-3236 enhanced sensitivity to paclitaxel in 8 of 10 cell lines, as well as in SKOv3ip (P = 0.028) and OVCAR8 xenografts.?In at least three cell lines, a synergistic interaction was observed.?ARN-3236 uncoupled the centrosome from the nucleus in interphase, blocked centrosome separation in mitosis, caused prometaphase arrest, and induced apoptotic cell death and tetraploidy.?ARN-3236 also inhibited AKT phosphorylation and attenuated survivin expression.
Cell Research	SIK2 expression was determined in ovarian cancer tissue samples and cell lines.?ARN-3236 was tested for its efficiency to inhibit growth and enhance paclitaxel sensitivity in cultures and xenografts of ovarian cancer cell lines.?SIK2 siRNA and ARN-3236 were compared for their ability to produce nuclear-centrosome dissociation, inhibit centrosome splitting, block mitotic progression, induce tetraploidy, trigger apoptotic cell death and reduce AKT/survivin signaling.

Molecular Weight	336.41
Formula	C19H16N2O2S
CAS No.	1613710-01-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 130 mg/mL (386.43 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Zhou J , Alfraidi A , Zhang S , et al. A novel compound ARN-3236 inhibits Salt Inducible Kinase 2 and sensitizes ovarian cancer cell lines and xenografts to paclitaxel[J]. Clinical Cancer Research, 2016:1078-0432.CCR-16-1562. 2. Liu Y, Tang W, Ji C, et al. The selective SIK2 inhibitor ARN-3236 produces strong antidepressant-like efficacy in mice via the hippocampal CRTC1-CREB-BDNF pathway[J]. Frontiers in pharmacology. 2020, 11.

Citations

1. Liu Y, Tang W, Ji C, et al. The selective SIK2 inhibitor ARN-3236 produces strong antidepressant-like efficacy in mice via the hippocampal CRTC1-CREB-BDNF pathway. Frontiers in pharmacology. 2020, 11. 2. Zou L, Hong D, Li K, et al. Salt-inducible kinase 2 (SIK2) inhibitor ARN-3236 attenuates bleomycin-induced pulmonary fibrosis in mice. BMC Pulmonary Medicine. 2022, 22(1): 1-11

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

ARN-3236 1613710-01-2 Chromatin/Epigenetic PI3K/Akt/mTOR signaling SIK AMPK inhibit ARN3236 Salt-inducible Kinase (SIK) ARN 3236 Inhibitor inhibitor

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