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CAS No.: 2593254-90-9

NSC622608 Catalog No. CSN32738

NSC622608 as the first small-molecule ligand for VISTA (V-domain Ig Suppressor of T-cell Activation) with IC50 value of 4.8 ± 0.4 μM (measured by FRET assay).

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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].
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实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1032 mL
- 15.5161 mL
- 31.0323 mL
- 5 mM
- 0.6206 mL
- 3.1032 mL
- 6.2065 mL
- 10 mM
- 0.3103 mL
- 1.5516 mL
- 3.1032 mL

技术信息

CAS号	2593254-90-9	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C9H12BrN3OS2	运输	蓝冰
分子量	322.25	别名

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