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NSC622608

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Chemical Structure| 2593254-90-9 同义名 : -
CAS号 : 2593254-90-9
货号 : A1489781
分子式 : C9H12BrN3OS2
纯度 : 99%+
分子量 : 322.245
MDL号 : MFCD34563797
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(124.13 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 12 mg/mL(37.24 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 V-domain Ig suppressor of T-cell activation (VISTA), which belongs to the B7 family and is expressed predominantly on hematopoetic cells, myeloid, granulocytic and T cells, can suppresses T-cell activation in vivo and vitro[1]. VISTA was highly expressed in human ovarian and endometrial cancers. Upregulation of VISTA in endometrial cancer was related to the methylation status of the VISTA promoter. VISTA in tumour cells suppressed T cell proliferation and cytokine production in vitro, and decreased the tumour-infiltrating CD8+ T cells in vivo. Anti-VISTA antibody prolonged the survival of tumour-bearing mice[2]. At cellular levels, VISTA regulated the effector functions of myeloid-derived suppressor cells and tolerogenic dendritic cell (DC) subsets. Blocking VISTA augmented their ability to produce proinflammatory mediators and diminished their T cell-suppressive functions[3].The levels of VISTA were positively associated with PD-L1, PD-1, CD8+ T cells and CD68+ macrophages. VISTA expression was higher in T-lymphocytes than in macrophages; and in cytotoxic T cells than in T-helper cells. Elevated VISTA was associated with absence of EGFR mutations and lower mutational burden in lung adenocarcinomas[4].VISTA is an immune checkpoint that affects the ability of T-cells to attack tumors. A FRET-based high throughput screening identified NSC622608 as the first small-molecule ligand for VISTA. Screening NSC622608 against a library of single-point VISTA mutants revealed the key residues in VISTA interacting with NSC622608. Further structural optimization resulted in a lead with submicromolar VISTA binding affinity. The lead compound blocked VISTA signaling in vitro, enhanced T-cell proliferation, and restored T-cell activation in the presence of VISTA-expressing cancer cell lines.[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.10mL

0.62mL

0.31mL

15.52mL

3.10mL

1.55mL

31.03mL

6.21mL

3.10mL
参考文献

[1]Ledi Kuang, Yuedong He. Potential value of V-domain Ig suppressor of T-cell activation for assessing progn osis in cervical cancer and as a target for therapy. Int J Clin Exp Pathol. 2020 Jan 1;13(1):26-37.

[2]Kumuluzi Mulati,et al. Br J Cancer. 2019 Jan;120(1):115-127.

[3]Wenwen Xu,et al. Immune-Checkpoint Protein VISTA Regulates Antitumor Immunity by Controlling Myeloid Cell-Mediated Inflammation and Immunosuppression. Cancer Immunol Res. 2019 Sep;7(9):1497-1510.

[4]Franz Villarroel-Espindola,et al. Spatially Resolved and Quantitative Analysis of VISTA/PD-1H as a Novel Immunotherapy Target in Human Non-Small Cell Lung Cancer. Clin Cancer Res. 2018 Apr 1;24(7):1562-1573.

[5]Moustafa T Gabr, et al. J Am Chem Soc. 2020 Sep 23;142(38):16194-16198.