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CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity.

For research use only. We do not sell to patients.

CD161 Chemical Structure

CD161 Chemical Structure

CAS No. : 1627716-22-6

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Description

CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity[1].

IC50 & Target

IC50: 28.2 nM (BRD4 BD1) and 7.2 nM (BRD4 BD2)[1]

Cellular Effect
Cell Line Type Value Description References
BT-20 IC50
1713 nM
Compound: 31
Cytotoxicity against human BT20 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human BT20 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
BT-474 IC50
434 nM
Compound: 31
Cytotoxicity against human BT474 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human BT474 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
BT-549 IC50
410 nM
Compound: 31
Cytotoxicity against human BT549 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human BT549 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
HBL-100 IC50
> 2000 nM
Compound: 31
Cytotoxicity against human HBL100 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human HBL100 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
HCC1143 IC50
> 2000 nM
Compound: 31
Cytotoxicity against human HCC1143 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human HCC1143 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
HCC1395 IC50
1233 nM
Compound: 31
Cytotoxicity against human HCC1395 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human HCC1395 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
HCC1937 IC50
> 2000 nM
Compound: 31
Cytotoxicity against human HCC1937 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human HCC1937 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
HCC1954 IC50
1604 nM
Compound: 31
Cytotoxicity against human HCC1954 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human HCC1954 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
HCC38 IC50
285 nM
Compound: 31
Cytotoxicity against human HCC38 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human HCC38 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
HCC70 IC50
1623 nM
Compound: 31
Cytotoxicity against human HCC70 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human HCC70 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
MDA-MB-157 IC50
39 nM
Compound: 31
Cytotoxicity against human MDA-MB-157 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human MDA-MB-157 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
MDA-MB-231 IC50
244 nM
Compound: 31
Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
MDA-MB-361 IC50
189 nM
Compound: 31
Cytotoxicity against human MDA-MB-361 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human MDA-MB-361 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
MDA-MB-436 IC50
1698 nM
Compound: 31
Cytotoxicity against human MDA-MB-436 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human MDA-MB-436 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
MDA-MB-453 IC50
188 nM
Compound: 31
Cytotoxicity against human MDA-MB-453 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human MDA-MB-453 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
MDA-MB-468 IC50
1018 nM
Compound: 31
Cytotoxicity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
MOLM-13 IC50
53 nM
Compound: 31
Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay
Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay
[PMID: 28463487]
MV4-11 IC50
26 nM
Compound: 31
Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay
Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay
[PMID: 28463487]
SUM149PT IC50
601 nM
Compound: 31
Cytotoxicity against human SUM149PT cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human SUM149PT cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
SUM-159-PT IC50
> 2000 nM
Compound: 31
Cytotoxicity against human SUM159PT cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human SUM159PT cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28463487]
In Vitro

CD161 (NKR-P1A) has Kis of 8.2 nM and 1.4 nM for BRD4 BD1 and BRD4 BD2, respectively[1].
CD161 (30-3000 nM; 1 hours) is very effective in inducing rapid down-regulation of c-Myc at as early as the 1 h time point and in a dose-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MV4;11 leukemia cells.
Concentration: 30, 100, 300, 1000, 3000 nM
Incubation Time: 1 hours
Result: Induced rapid down-regulation of c-Myc at as early as the 1 hours time point and in a dose-dependent manner.
In Vivo

CD161 (NKR-P1A) (po; 20, 40 mg/kg/day; 45 days) achieves essentially complete tumor growth inhibition[1].
CD161 (5 mg/kg (iv), 25 mg/kg (po); 0-24 hours) has the t1/2 of 2.4 hours (iv) and 2.9 hours (po) for rat; the Cmax of 7333 ng/mL (po) for rat. The t1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the Cmax of mice is 983.1 ng/mL (po) [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Dorsal side of severe combined immunodeficient (SCID) mice[1]
Dosage: 20, 40 mg/kg
Administration: Po; daily; 45 days
Result: Achieved essentially complete tumor growth inhibition.
Animal Model: Rat or mice[1]
Dosage: 5 mg/kg (iv), 25 mg/kg (po) for rat and mice (Pharmacokinetic Study)
Administration: Iv and po; 0, 5, 15, 30 mins, and 1, 2, 4, 6, 8, 24 hours
Result: The t1/2 of rat is 2.4 hours (iv) and 2.9 hours (po); the Cmaxof rat is 7333 ng/mL (po). The t1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the Cmax of mice is 983.1 ng/mL (po) [1].
Molecular Weight

435.48

Formula

C26H21N5O2

CAS No.
SMILES

CC1=NC(C2=CC=NC3=CC=CC=C23)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CD161
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