CA3(CIL56)

Name: CA3(CIL56)
Brand: Selleck Chemicals
SKU: S8661
Rating: 5 (1 reviews)

For research use only.

Catalog No.S8661

1 publication

Molecular Weight(MW): 489.61

CA3 has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties.

Selleck's CA3(CIL56) has been cited by 1 publication

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

PubMed: 31383722

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Biological Activity

Description

CA3 has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties.

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	NW\pcIZjTnWwY4Tpc44h[XO\|YYm=				M1TBVWlvcGmkaYTpc44hd2ZiV370M4JmfGFvY3H0[Y5qdiC2cnHud4NzcXC2aX;uZYwh[WO2aY\peJkhcW5iaIXtZY4hUFRvMkmgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVxdGW2aX;uJI9nKGKndHGtZ4F1\W6rbjDs[ZZmdCCkeTDUR2YhdHWlaX\ldoF{\SCycn;tc5RmeiC{ZYDvdpRmeiCjc4Phfg+9lCCLQ{WwQVAvQTlizszN	MmjjNlYyQDJ{M{i=

... 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]

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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
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	O/N=C1/C2=CC(=CC=C2C3=C1C=C(C=C3)[S](=O)(=O)N4CCCCC4)[S](=O)(=O)N5CCCCC5

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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 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.
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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)