Diprovocim_product_DataBase

Bioactivity

Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses[1][2].

Invitro

Diprovocim (在 THP-1 细胞中为 5 nM, 在小鼠腹膜巨噬细胞中为 500 nM; 15-120 分钟) 诱导 IKKα、IKKβ、p38、JNK 和 ERK 的磷酸化，以及 IκBα 的降解[2]。 Diprovocim (0.01-10000 nM; 4 小时) 诱导 THP-1 细胞 (EC50=110 pM)、人外周血单核细胞 (PBMC) (EC50=875 pM) 和小鼠腹腔巨噬细胞 (EC50=1.3 nM) 和骨髓来源的树突状细胞 (BMDC) (EC50=6.7 nM) 产生剂量依赖性 TNF。除 TNF 外，Diprovocim 还诱导小鼠 BMDC 产生 IL-6[2]。 Western Blot Analysis[2] Cell Line:

In Vivo

Diprovocim (10 mg/kg) 用作佐剂，在与卵清蛋白 (OVA; 100 μg) 混合并肌肉注射，14 天后检测发现可以诱导相似水平的血清 OVA 特异性 IgG[2]。 Diprovocim (10 mg/kg) 与卵清蛋白 (OVA; 100 μg) 混合后，在接种 B16-OVA 细胞免疫前进行肌肉注射，可以显着减缓肿瘤生长速度[2]。 Animal Model:

Name

Diprovocim

CAS

2170867-89-5

Formula

C56H56N6O6

Molar Mass

909.08

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

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

Reference

[1]. Matthew D Morin, et al. Diprovocims: A New and Exceptionally Potent Class of Toll-like Receptor Agonists. J Am Chem Soc. 2018 Oct 31;140(43):14440-14454. [2]. Ying Wang, et al. Adjuvant effect of the novel TLR1/TLR2 agonist Diprovocim synergizes with anti-PD-L1 to eliminate melanoma in mice. Proc Natl Acad Sci U S A. 2018 Sep 11;115(37):E8698-E8706.

PeptideDB

Diprovocim

CAS: 2170867-89-5 F: C56H56N6O6 W: 909.08