An inhibitor of SIK2 (IC50 = 50s = 21.63 and 6.63 nM

ARN3236 – 10 mg

Brand:
Cayman
CAS:
1613710-01-2
Storage:
-20
UN-No:
Non-Hazardous - /

ARN3236 is an inhibitor of salt-inducible kinase 2 (SIK2; IC50 = 50s = 21.63 and 6.63 nM, respectively). It inhibits TNF-α secretion in RAW 264.7 cells (IC50 = ~2.5 µM) and reduces phosphorylation of the SIK2 targets CRTC3 and HDAC4 in macrophages when used at a concentration of 3 µM. ARN3236 inhibits growth of 10 ovarian cancer cell lines (IC50s = 0.8-2.6 µM) and increases the sensitivity of eight of them to paclitaxel (Item No. 10461).{54419} It halts the cell cycle at the G2/M phase and induces apoptosis and tetraploidy in SKOV3 cells when used at a concentration of 1 µM. ARN3236 (60 mg/kg per day) has an additive effect on reducing tumor growth when used in combination with paclitaxel in an ovarian cancer mouse xenograft model.  

 

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SKU: 31457 - 10 mg Category:

Description

An inhibitor of SIK2 (IC50 = 50s = 21.63 and 6.63 nM, respectively); inhibits TNF-α secretion in RAW 264.7 cells (IC50 = ~2.5 µM) and reduces phosphorylation of CRTC3 and HDAC4 in macrophages at 3 µM; inhibits growth of 10 ovarian cancer cell lines (IC50s = 0.8-2.6 µM) and increases sensitivity of eight of them to paclitaxel; halts the cell cycle at the G2/M phase and induces apoptosis and tetraploidy in SKOV3 cells at 1 µM; has an additive effect on reducing tumor growth when used in combination with paclitaxel in an ovarian cancer mouse xenograft model at 60 mg/kg per day

Formal name: 3-(2,4-dimethoxyphenyl)-4-(3-thienyl)-1H-pyrrolo[2,3-b]pyridine

Synonyms: 

Molecular weight: 336.4

CAS: 1613710-01-2

Purity: ≥98%

Formulation: A crystalline solid

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