cyclo(RLsKDK) TFA_product_DataBase

Bioactivity

cyclo(RLsKDK) (TFA) (BK-1361 (TFA)) is a specific inhibitor of metalloproteinase ADAM8 with an IC50 value of 182 nM. cyclo(RLsKDK) (TFA) has potential applications in inflammatory diseases and cancer[1].

Invitro

cyclo(RLsKDK) (TFA) 促使 ADAM8 激活和 CD23 脱落，IC50 值分别为 120 nM 和 182 nM。cyclo(RLsKDK) (TFA) (200 nM；0-120 h) 增加了 pro-ADAM8 的活性[2]。cyclo(RLsKDK) (TFA) (200 nM and 500 nM；12 h) 促进了 Panc1_ctrl 和 Panc1_A8 细胞的生长[2]。cyclo(RLsKDK) (TFA) (500 nM) 导致 Panc1_ctrl 和 Panc1_A8 细胞中 ERK1/2 磷酸化[2]。 Cell Invasion Assay[2] Cell Line:

In Vivo

cyclo(RLsKDK) (TFA) (10 µg/g；腹腔注射；一周一次持续 4 周) 显著降低了植入 Panc1_ctrl 或 Panc1_A8 细胞的小鼠中的肿瘤量。cyclo(RLsKDK) (TFA) 提高了胰腺导管腺癌 (PDAC) 小鼠存活率，降低了可溶性 ADAM8 (sADAM8) 含量、pERK1/2 活化、PDAC 在 PDAC 小鼠肝脏和肺部中的转移[2]。

Name

cyclo(RLsKDK) TFA

Sequence

Cyclo(Arg-Leu-{d-Ser}-Lys-Asp-Lys)

Shortening

Cyclo(RL-{d-Ser}-KDK)

Formula

C33H58F3N11O11

Molar Mass

841.88

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light, under nitrogen

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

Reference

[1]. Yim V, et al. Synthesis and biological evaluation of analogues of the potent ADAM8 inhibitor cyclo(RLsKDK) for the treatment of inflammatory diseases and cancer metastasis. Bioorg Med Chem. 2016 Sep 15;24(18):4032-4037. [2]. Schlomann U, et al. ADAM8 as a drug target in pancreatic cancer. Nat Commun. 2015 Jan 28;6:6175.

PeptideDB

cyclo(RLsKDK) TFA

CAS: F: C33H58F3N11O11 W: 841.88