SQ22536

Catalog No.S8283 Batch:S828301

Technical Data

Formula	C₉H₁₁N₅O
Molecular Weight	205.22	CAS No.	17318-31-9
Solubility (25°C)*	In vitro	DMSO	41 mg/mL (199.78 mM)
		Water	41 mg/mL (199.78 mM)
		Ethanol	41 mg/mL (199.78 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

SQ22536 (9-(tetrahydrofuran-2-yl)-9h-purin-6-amine) is an inhibitor of adenylyl cyclase with an IC50 of 1.4 μM. It can inhibit PGE1-stimulated increases in cAMP levels in intact human platelets.

Targets

Adenylyl cyclase ^[1]

In vitro

SQ22536(250 µmol/L) attenuates the inhibitory effect of adenosine against ADP-induced platelet aggregation from 8±5 to 57±5%, respectively (p<0.001). SQ22536 also attenuates an increase of intraplatelet levels of cAMP by adenosine from 29±2 to 9±1 pmol/108 platelets (p<0.05). It has no effect on the platelet antiaggregant activity of inosine (1 to 4 mmol/L) and ADP-induced platelet aggregation^[4].

In vivo

SQ22536 abolishes the renal protective effects in KK/Ta-Akita mice. the amelioration of glomerular histopathological damage is eliminated in KK/Ta-Akita mice treated with SQ22536. Renal cAMP does not increase after treatment with SQ22536. In a word, the beneficial actions for treatment of nephropathy are inhibited by the adenylate cyclase inhibitor SQ22536^[5].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Human leukemic mast cell line(HMC-1) and human umbilical cord blood-derived mast cell(hCBMCs) Concentrations 0.1, 1, 10 mM Incubation Time 30 min Method HMC-1 cells and hCBMCs are plated in 48-well plates and serum-starved overnight. The next day, cells are preincubated with SQ22536 at the indicated concentrations for 30 min before stimulation with CRH (100 nM for HMC-1 or 1 μM for hCBMC) for 3 min in the presence or absence of SQ22536 in serum-free culture media. Cell lysates are then prepared and assayed for protein kinase A activity using ELISA.
Animal Study:^{^[3]}	Animal Models Male C57BL/6J mice Dosages 10 mg/kg Administration s.c.

Cell Assay:^{^[2]}

Cell lines
Human leukemic mast cell line(HMC-1) and human umbilical cord blood-derived mast cell(hCBMCs)
Concentrations
0.1, 1, 10 mM
Incubation Time
30 min
Method
HMC-1 cells and hCBMCs are plated in 48-well plates and serum-starved overnight. The next day, cells are preincubated with SQ22536 at the indicated concentrations for 30 min before stimulation with CRH (100 nM for HMC-1 or 1 μM for hCBMC) for 3 min in the presence or absence of SQ22536 in serum-free culture media. Cell lysates are then prepared and assayed for protein kinase A activity using ELISA.

Animal Study:^{^[3]}

Animal Models
Male C57BL/6J mice
Dosages
10 mg/kg
Administration
s.c.

References

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Customer Product Validation

: Data from [Data independently produced by , , ONCOLOGY REPORTS, 2017, 37:3572-3580]

: Data from [Data independently produced by , , J Food Sci, 2018, 83(9):2394-2401]

Selleck's SQ22536 has been cited by 23 publications

Promoting collateral formation in type 2 diabetes mellitus using ultra-small nanodots with autophagy activation and ROS scavenging [ J Nanobiotechnology, 2024, 22(1):85]	PubMed: 38429826
NEAT1 Deficiency Promotes Corneal Epithelial Wound Healing by Activating cAMP Signaling Pathway [ Invest Ophthalmol Vis Sci, 2024, 65(3):10]	PubMed: 38466291
Suppression of cAMP/PKA/CREB signaling ameliorates retinal injury in diabetic retinopathy [ Kaohsiung J Med Sci, 2023, 10.1002/kjm2.12722]	PubMed: 37338034
ACE2 pathway regulates thermogenesis and energy metabolism [ Elife, 2022, 11e72266]	PubMed: 35014608
Regulation of CRE-Dependent Transcriptional Activity in a Mouse Suprachiasmatic Nucleus Cell Line [ Int J Mol Sci, 2022, 23-2012226]	PubMed: 36293078
Atorvastatin inhibits neuronal apoptosis via activating cAMP/PKA/p-CREB/BDNF pathway in hypoxic-ischemic neonatal rats [ FASEB J, 2022, 36(4):e22263]	PubMed: 35303316
Targeting adipocytic discoidin domain receptor 2 impedes fat gain while increasing bone mass [ Cell Death Differ, 2021, 10.1038/s41418-021-00887-9]	PubMed: 34645939
FOSL2 promotes VEGF-independent angiogenesis by transcriptionnally activating Wnt5a in breast cancer-associated fibroblasts [ Theranostics, 2021, 11(10):4975-4991]	PubMed: 33754039
Conjugated secondary 12α-hydroxylated bile acids promote liver fibrogenesis [ EBioMedicine, 2021, 66:103290]	PubMed: 33752128
Microglial MT1 activation inhibits LPS-induced neuroinflammation via regulation of metabolic reprogramming [ Aging Cell, 2021, e13375]	PubMed: 33964119

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.