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CASIN

SKU: orb1223127

Description

CASIN is an inhibitor of Cdc42 GTPase, a small GTPase of the Rho-subfamily that plays important roles in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. CASIN generated a rejuvenated phenotype of Hematopoietic stem cells (HSCs), reversing the aging-related and polarity phenotype of aged HSCs to that of young HSCs in vivo.

Images & Validation

Key Properties

CAS Number425399-05-9
MW306.41
Purity>98% (HPLC)
FormulaC20H22N2O
SMILESC1CC(c2c(C1)c1c([nH]2)ccc(c1)c1ccccc1)NCCO
TargetIntegrin
SolubilityDMSO : ≥ 31 mg/mL; 101.17 mM

Bioactivity

In Vivo
CASIN (20 mg/kg; i.p. 2 times a day) prolongs lifetime of mice with busulfan injection. Animal model: NSG mice with busulfan injection. Dosage: 20 mg/kg. Administration: Intraperitoneal injection; 20 mg/kg 2 times a day. Result: Significantly prolonged the lifespan of xenografts mice better than bortezomib, and showed a leading position when combined with bortezomib.
In Vitro
CASIN (0-10 μM; 3 d) inhibits the growth of AMO-1, ARH-77, IM-9, JJN-3, L-363, MOLP-8 and RPMI-8226/S cells. CASIN (0-10 μM; 16 h) inhibits melphalan induced FANCD2 mono-ubiquitination in LR5 cells but shows no effect to S cells. CASIN (5 μM; 2 d) increases cell apoptosis of bortezomib-resistant MM patient cells. Cell Viability Assay Cell line: AMO-1, ARH-77, IM-9, JJN-3, L-363, MOLP-8 and RPMI-8226/S cells. Concentration: 0-10 μM. Incubation time: 3 days. Result: Inhibited MM cell lines including AMO-1, ARH-77, IM-9, JJN-3, L-363, MOLP-8 and RPMI-8226/S cells with GI50s vof 3.23, 4.31, 4.87, 2.56, 4.64, 4.67 and 3.97 μM, respectively. Western blot analysis. Cell line: MM (S) and melphalan-resistant (LR5) MM cells. Concentration: 5 μM. Incubation time: 16 hours. Result: Abolished melphalan induced FANCD2 mono-ubiquitination and DNA damage in LR5, sensitized LR5 to melphalan-induced cell death by blocking FANCD2-mediated DNA damage repair. Apoptosis Analysis Cell line: Bortezomib-resistant MM patients cells. Concentration: 5 μM. Incubation time: 2 days. Result: 2-fold increased cell apoptosis in the cell derived from bortezomib-resistant MM patients.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

CASIN

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CASIN (orb1223127)

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Available Sizes

Select a size below

2 mg
¥ 1,170.00
5 mg
¥ 1,560.00
10 mg
¥ 2,470.00
25 mg
¥ 3,770.00
50 mg
¥ 5,330.00
100 mg
¥ 8,060.00
500 mg
¥ 16,770.00