BMS-1 is an inhibitor of the PD-1/PD-L1 protein/protein interaction (IC₅₀ between 6 and 100 nM)^[1][2].

PD1-PDL1^[1]

Since PD-1 mediated the exhaustion of natural killer (NK) cell by binding to its ligand PD-L1, BMS-1 (PD-1/PD-L1 inhibitor 1) (1 μM, 3 days) is used to disturb the interaction between PD-1 and PD-L1. Dexamethasone induced increase of PD-1 expression and decrease of cytotoxicity of the co-cultured NK92 cells are reversed by BMS-1^[1]. BMS-1, a small-molecule immune checkpoint inhibitor of PD-1/PD-L1, can be used as a therapeutic strategy for tumor immunotherapy^[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.

BMS-1 (500 μg/mL; 100 μL; i.p.) significantly increases the survival rates of the mVEGF165b group and mVEGF165b + MUC1 group^[3].

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.

475.58

C₂₉H₃₃NO₅

1675201-83-8

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

Methanol : 25 mg/mL (52.57 mM; Need ultrasonic)

DMSO : 17.86 mg/mL (37.55 mM; ultrasonic and warming and heat to 60°C)

DMF : 5 mg/mL (10.51 mM; Need ultrasonic)

*

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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 1 mg/mL (2.10 mM); Clear solution

  此方案可获得 ≥ 1 mg/mL (2.10 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 1 mg/mL (2.10 mM); Clear solution

  此方案可获得 ≥ 1 mg/mL (2.10 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 1 mg/mL (2.10 mM); Clear solution

  此方案可获得 ≥ 1 mg/mL (2.10 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Zhao Y, et al. Depression Promotes Hepatocellular Carcinoma Progression through a Glucocorticoids Mediated Up-Regulation of PD-1 Expression in Tumor infiltrating NK Cells. Carcinogenesis. 2019 Feb 4.

  [2]. Li K, et al. Development of small-molecule immune checkpoint inhibitors of PD-1/PD-L1 as a new therapeutic strategy for tumour immunotherapy. J Drug Target. 2019 Mar;27(3):244-256.

  [3]. Zhang H, et al. Utilizing VEGF165b mutant as an effective immunization adjunct to augment antitumor immune response. Vaccine. 2019 Apr 3;37(15):2090-2098.

  [4]. Mengyuan Li, et al. KALRN mutations promote antitumor immunity and immunotherapy response in cancer. J Immunother Cancer. 2020 Oct;8(2):e000293.