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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

Pack Size	Availability	Price/USD
1 mg	In stock	$ 55.00
2 mg	In stock	$ 78.00
5 mg	In stock	$ 126.00
10 mg	In stock	$ 192.00
25 mg	In stock	$ 360.00
50 mg	In stock	$ 450.00
100 mg	In stock	$ 693.00
200 mg	In stock	$ 987.00
500 mg	In stock	$ 1,460.00
1 mL * 10 mM (in DMSO)	In stock	$ 153.00

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Purity: 99.7%

Purity: 99.57%

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	SIK1:21.63 nM , SIK2:<1 nM , SIK3:6.63.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 1 year

Solubility Information

DMSO: 130 mg/mL (386.43 mM)

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

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Preclinical Compound Library Anti-Metabolism Disease Compound Library Bioactive Compound Library Anti-Obesity Compound Library Lipid Metabolism Compound Library Anti-Diabetic Compound Library Neuronal Differentiation Compound Library

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Keywords

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

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