Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma[1][2].
IC50 & Target
Ki: 31 nM (LSD1)[1] IC50: 13 nM (LSD1)[1]
体外研究 (In Vitro)
Seclidemstat (72 hours) mesylate inhibits SWI/SNF-mutation-dependent tumor cell proliferation with IC50 ranging from 0.013 to 2.819 μM (COV434, BIN67, SCCOHT-1, TOV21G, SKOV3, A427, H522, A549, H1299, G401, G402, HCC15 cells)[2]. Seclidemstat (72 hours) mesylate promotes endogenous retroviruses (ERVs) expression and activation of IFNβ pathway in SCCOHT cell lines (SCCOHT-1, BIN67, and COV434 cells)[2]. Seclidemstat (3 μM) mesylate promotes PD-L1 expression in SCCOHT COV 434 pIND 20 BRG1-2.7 cell line[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
547.04
Formula
C21H27ClN4O7S2
CAS 号
2044953-70-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:
DMSO : 53.33 mg/mL (97.49 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
1.8280 mL
9.1401 mL
18.2802 mL
5 mM
0.3656 mL
1.8280 mL
3.6560 mL
10 mM
0.1828 mL
0.9140 mL
1.8280 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
参考文献
[1]. Dai XJ, et al. Reversible Lysine Specific Demethylase 1 (LSD1) Inhibitors: A Promising Wrench to Impair LSD1 [published correction appears in J Med Chem. 2021 May 13;64(9):6410-6411]. J Med Chem. 2021;64(5):2466-2488.
[2]. Soldi R, et al. The novel reversible LSD1 inhibitor SP-2577 promotes anti-tumor immunity in SWItch/Sucrose-NonFermentable (SWI/SNF) complex mutated ovarian cancer. PLoS One. 2020;15(7):e0235705. Published 2020 Jul 10.
SP-96 is a highly potent, selective and non-ATP-competitive Aurora B (IC50=0.316 nM) inhibitor and shows >2000 fold selectivity against FLT3 and KIT. SP-96 shows selective growth inhibition in NCI60 screening, incluing MDA-MD-468 (GI50=107 nM). SP-96 can be used for the research of triple negative breast cancer (TNBC)[1].
IC50 & Target[1]
Aurora A
18.975 nM (IC50)
Aurora B
0.316 nM (IC50)
体外研究 (In Vitro)
SP-96 is a highly potent, selective and non-ATP-competitive Aurora B (IC50=0.316 nM) inhibitor and shows >2000 fold selectivity against FLT3 (IC50=1475.6 nM) and KIT (IC50=1307.6 nM)[1].SP-96 (0-1 µM; 24 hours) is not promiscuous, rather selective for a few cell lines, it inhibits MDA-MB-468, CCRF-CEM, COLO 205 and A498 cell growth with GI50 values of 107 nM,47.4 nM, 50.3 nM and 53.2 nM, respectively[1].SP-96 (63.2 nM) inhibits Aurora B activity in H460 cells by the characteristics of increased DNA content, and it increases cell volume with enormous nucleus[1].SP-96 (0-2 µM) inhibits Aurora B enzymatic activity with an IC50 of 0.316 nM and inhibits Aurora A with observed IC50 value of 18.975 nM. SP-96 shows >2000 fold selectivity against FLT3 (IC50=1475.6 nM) and KIT (IC50=1307.6 nM). Meanwhile, it exhibits inhibitory effects on other receptor tyrosine kinases (RTKs) namely EGFR, RET and HER2 with IC50 value ≥2 µM[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
MDA-MB-468, CCRF-CEM, COLO 205 and A498 cell
Concentration:
0-1 µM
Incubation Time:
24 hours
Result:
Showed good inhibitory activity on MDA-MB-468 cells.
分子量
453.47
Formula
C25H20FN7O
CAS 号
2682114-54-9
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Naga Rajiv Lakkaniga,et al. Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression.Eur J Med Chem. 2020 Jul 12;203:112589.
2B-(SP) TFA is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) TFA is readily phosphorylated by both the α and β isoforms of GSK-3[1].
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. G I Welsh, et al. Peptide substrates suitable for assaying glycogen synthase kinase-3 in crude cell extracts.Anal Biochem. 1997 Jan 1;244(1):16-21.