ZCL278

Biological Activity

ZCL278 is a selective Cdc42 GTPase inhibitor with K_d of 11.4 μM.

Product Citations

• 

  Adv Sci (Weinh). 2022 Jul;9(21):e2201414.

  Bile Acid Conjugation on Solid Nanoparticles Enhances ASBT‐Mediated Endocytosis and Chylomicron Pathway but Weakens the Transcytosis by Inducing Transport
  ZCL278 purchased from AbMole

• 

  Int J Pharm. 2022 Feb 14;617:121589.

  Lipid raft-mediated and upregulated coordination pathways assist transport of glycocholic acid-modified nanoparticle in a human breast cancer cell line of SK-BR-3
  ZCL278 purchased from AbMole

• 

  Int J Nanomedicine. 2018 Jul 27;13:4391-4404.

  Rho GTPases in A549 and Caco-2 cells dominating the endocytic pathways of nanocarbons with different morphologies.
  ZCL278 purchased from AbMole

• 

  ACS Appl Mater Interfaces. 2017 Feb 22;9(7):5803-5816.

  Transmembrane Pathways and Mechanisms of Rod-like Paclitaxel Nanocrystals through MDCK Polarized Monolayer
  ZCL278 purchased from AbMole

Customer Product Validations & Biological Datas

	Source	International Journal of Nanomedicine (2018). Figure 5. ZCL278 (Abmole Bioscience, Houston, TX, USA)
	Method	RNA interference
	Cell Lines	A549 cells
	Concentrations
	Incubation Time	24 h
	Results	These findings indicated that Cdc42 played a vital role in the uptake of oxMWCNTs in A549 cells, while Rac1 and RhoA might not be involved in this process.

	Source	ACS Appl Mater Interfaces (2017). Figure 9. ZCL 278 (Abmole BioScience. Houston, TX, USA)
	Method	Transwells
	Cell Lines	MDCK cells
	Concentrations
	Incubation Time
	Results	As shown in Figure 9, in the presence of ZCL 278, the transmembrane amount of PTX-NCs was reduced significantly, indicating that Cdc 42 participated in the regulation of the transport of PTX-NCs.

Chemical Information

Molecular Weight	584.89
Formula	C21H19BrClN5O4S2
CAS Number	587841-73-4
Solubility (25°C)	DMSO 70 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

Conversion of different model animals based on BSA (PMID: 27057123)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Natasha P Murphy, et al. Progress in the therapeutic inhibition of Cdc42 signalling

[2] Xiaoyan Li, et al. Intersectin-Cdc42 interaction is required for orderly meiosis in porcine oocytes

[3] Yi-Ying Chou, et al. Identification and Characterization of a Novel Broad-Spectrum Virus Entry Inhibitor

[4] Xiaona Liu, et al. Neuroglobin Plays a Protective Role in Arsenite-Induced Cytotoxicity by Inhibition of Cdc42 and Rac1GTPases in Rat Cerebellar Granule Neurons

[5] Amy Friesland, et al. Small molecule targeting Cdc42-intersectin interaction disrupts Golgi organization and suppresses cell motility