CA3 (CIL56)

Name: CA3 (CIL56)
Brand: Selleck Chemicals
SKU: S8661
Rating: 5 (7 reviews)

For research use only.

Catalog No.S8661

7 publications

CAS No. 300802-28-2

CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces ferroptosis and iron-dependent reactive oxygen species (ROS).

Selleck's CA3 (CIL56) has been cited by 7 publications

Clin Cancer Res, 2020, clincanres.0018.2020

PubMed: 33172899 ( click the link to review the publication )

J Neurosci, 2020, 13;40(20):3915-3932

PubMed: 32341094 ( click the link to review the publication )

Am J Transl Res, 2020, 12(10):6490-6500

PubMed: 33194046 ( click the link to review the publication )

Exp Biol Med (Maywood), 2020, 1535370220977101

PubMed: 33307801 ( click the link to review the publication )

Artif Cells Nanomed Biotechnol, 2020, 48(1):920-932

PubMed: 32496895 ( click the link to review the publication )

FASEB J, 2019, 33(6):7143-7154

PubMed: 30844312 ( click the link to review the publication )

Mol Cancer Res, 2019, 17(10):2029-2041

PubMed: 31383722 ( click the link to review the publication )

Purity & Quality Control

Choose Selective YAP Inhibitors

Biological Activity

Description

CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces ferroptosis and iron-dependent reactive oxygen species (ROS).

Targets

YAP/TEAD interaction ^[1]
()

In vitro

CA3 strongly inhibits esophageal adenocarcinoma cell growth in vitro. CA3 can effectively suppress tumor cell proliferation, induce apoptosis, reduce tumor sphere formation, and the population of ALDH1+ cells. CA3 specially inhibits Tead/YAP1 transcriptional activity but shows no inhibitory activity on other transcriptional factors-Super-TOP/Wnt, CBF1/Notch, and AP-1 after cotransfection of their respective individual promoter luciferases in 293T cells. CA3 preferentially inhibits CSC properties enriched in radiation-resistant esophageal adenocarcinoma cells^[1].

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
HT-29 cells	NWfFbndRTnWwY4Tpc44h[XO\|YYm=				MkTNTY5pcWKrdHnvckBw\iCZboSvZoV1[S2lYYTlcolvKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fUBqdiCqdX3hckBJXC1{OTDj[YxteyCjc4Pld5Nm\CCjczDk[ZBt\XSrb36gc4Yh[mW2YT3jZZRmdmmwIHzleoVtKGK7IGTDSkBtfWOrZnXyZZNmKHC{b33veIVzKHKncH;yeIVzKGG\|c3H589yNKEmFNUC9NE46QSEQvF2=	NYe0SZpZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xPFIzOzhpPkK2NVgzOjN6PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	YAP1 / SOX9 ; PubMed: 29167315 Mol Cancer Ther Cell lysate from SKGT-4 and JHESO EAC cells treated with CA3 at indicated dosage were selected for immunoblotting analysis for YAP1 and SOX9.	29167315
Immunofluorescence	YAP1 / SOX9 ; PubMed: 29167315 Mol Cancer Ther Immunofluorescent staining of YAP1 and SOX9 in JHESO cells were observed by confocal microscopy (right).	29167315
Growth inhibition assay	Cell viability; PubMed: 29167315 Mol Cancer Ther Four EAC cell lines A.SKGT-4, Flo-1,JHESO and OACP EAC cell lines were treated with 0.1% DMSO (as control), CA3 (left) at dosage of 0.1, 0.5 and 1µM, the cells proliferation and viability were measured using MTS assay and calculated as percent of control. B. SKGT-4 (PINYAP120) cells with (DOX+) or without (DOX−) YAP1 induction were treated with 0.1% DMSO (as control), CA3 (left) at dosage of 0.1, 0.5 and 1µM, the cells proliferation and viability were measured using MTS assay and calculated as percent of control. For all experiments, values shown represent the mean and SD of at least triplicate assays.**P<0.01.	29167315

In vivo

CA3 exerts strong antitumor activity in xenograft model with no apparent toxicity^[1].

Protocol

Cell Research:

^[1]

- Collapse

Cell lines: SKGT-4 and JHESO cells
Concentrations: 0.5 and 1 μmol/L
Incubation Time: 48 hours
Method:
SKGT-4 and JHESO cells are seeded onto 6-well plates (1 × 10⁵/well) in DMEM and cultured for 24 hours to allow for cell attachment. The cells are then treated with 0.1% DMSO (control) or CA3 at different doses as indicated for 48 hours. Next, the cells are harvested, fixed with methanol, washed, treated with RNase A, and stained for DNA with propidium iodide, and their DNA histograms and cell-cycle phase distributions are analyzed using flow cytometry.

(Only for Reference)

References

[1] Song S, et al. Mol Cancer Ther. 2018, 17(2):443-454.

Solubility (25°C)

In vitro	DMSO	97 mg/mL (198.11 mM)
	Water	Insoluble
	Ethanol	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download CA3 (CIL56) SDF

Molecular Weight	489.61
Formula	C₂₃H₂₇N₃O₅S₂
CAS No.	300802-28-2
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	C1CCN(CC1)S(=O)(=O)C2=CC3=C(C=C2)C4=C(C3=NO)C=C(C=C4)S(=O)(=O)N5CCCCC5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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The Serial Dilution Calculator Equation

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Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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CA3 (CIL56)