Art. -Nr.: HY-100830

NCB-0846

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

NCB-0846 is an orally active, selective inhibitor for Wnt, that inhibits Traf2- and Nck-interacting kinase (TNIK) with an IC₅₀ of 21 nM. NCB-0846 blocks TGF-β signaling pathway by inhibiting SMAD2/3 phosphorylation and nuclear translocation.

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Reinheit: 99.61%
CAS. Nr.: 1792999-26-8
Formel: C₂₁H₂₁N₅O₂
Molecular Weight:375.42

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

NCB-0846 Chemical Structure

CAS. Nr.: 1792999-26-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Wnt	TNIK 21 nM (IC₅₀)

Alle Wnt Isoform-spezifische Produkte anzeigen :

Alle MAP4K Isoform-spezifische Produkte anzeigen :

Alle TGF-beta/Smad Isoform-spezifische Produkte anzeigen :

Smad1
Smad3

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.09 μM Compound: NCB-0846	Inhibition of cell growth in human HCT-116 cells after 72 hrs by CCK-8 assay Inhibition of cell growth in human HCT-116 cells after 72 hrs by CCK-8 assay	[PMID: 38422698]
HCT-116	IC₅₀	0.4 μM Compound: NCB-0846	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 34985886]
HCT-116	IC₅₀	0.403 μM Compound: NCB-0846	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35447345]

In Vitro

NCB-0846 has anti-Wnt activity. NCB-0846 binds to TNIK in an inactive conformation, and this binding mode seems to be essential for Wnt inhibition. NCB-0846 shows inhibitory activity against TNIK with an IC₅₀ of 21 nM. NCB-0846 also inhibits FLT3, JAK3, PDGFRα, TRKA, CDK2/CycA2, and HGK. NCB-0846 induces faster migration of TCF4 phosphorylated by TNIK within a concentration range of 0.1-0.3 μM and completely inhibits the phosphorylation of TCF4 at a concentration of 3 μM. NCB-0846 inhibits HCT116 cell growth and shows much higher (-20-fold) inhibitory activity against colony formation by the same cells in soft agar^[1].

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

In Vivo

NCB-0846 suppresses the growth of tumors established by inoculating HCT116 cells into immunodeficient mice. The expression of Wnt-target genes (AXIN2, MYC and CCND1) in xenografts is reduced following the administration of NCB-0846. NCB-0846 induces an increase in the sub-G1 cell population. Cleavage of poly (ADP-ribose) polymerase 1 indicates the induction of apoptosis^[1].

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

Chemical Information

CAS. Nr. 1792999-26-8
Appearance Solid
Molecular Weight 375.42
Formel C₂₁H₂₁N₅O₂
Color Light yellow to yellow
SMILES

O[C@@H](CC1)CC[C@@H]1OC2=CC=CC(C=N3)=C2N=C3NC4=CC=C(N=CN5)C5=C4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (4)

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Journal Impact Factor

Sci Adv

TNIK: A redox sensor in endothelial cell permeability. [Abstract]

2024 Dec 20;10(51):eadk6583. PMID: 39705357
Cancer Lett

BET protein-dependent E2F pathway activity confers bell-shaped type resistance to tankyrase inhibitors in APC-mutated colorectal cancer. [Abstract]

2024 Mar 1:584:216632. PMID: 38216082
Oncogene

CRISPR screens identify a novel combination treatment targeting BCL-XL and WNT signaling for KRAS/BRAF-mutated colorectal cancers. [Abstract]

2021 May;40(18):3287-3302. PMID: 33846570

NCB-0846 purchased from MedChemExpress. Usage Cited in: Oncogene. 2021 May;40(18):3287-3302. [Abstract]

ABT-263 had negligible effects on MCL1 mRNA levels; however, treatment with NCB-0846 alone, as well as its combination with ABT-263, resulted in a significant decrease in MCL1 mRNA levels.
ACS Comb Sci

Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]

2019 Dec 9;21(12):805-816. PMID: 31689077

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 30 mg/mL (79.91 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6637 mL

13.3184 mL

26.6368 mL

5 mM

0.5327 mL

2.6637 mL

5.3274 mL

10 mM

0.2664 mL

1.3318 mL

2.6637 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.25 mg/mL (5.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.25 mg/mL (5.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Animal Administration^[1]

Mice: NCB-0846 is suspended in DMSO/polyethylene glycol#400/30% 2-hydroxypropyl-β-cyclodextrin solution (10:45:45v/v). Five million HCT116 cells suspended in medium containing 25% Matrigel are inoculated into the subcutaneous tissues of 9-week-old female BALB/c nude mice. Mice are randomized according to tumour volume (9 mice per group). NCB-0846 was administered daily by oral gavage at 0 (vehicle alone), 40 or 80 mg/kg (body weight) BID (bis in die) for 14 days^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Masuda M, et al. TNIK inhibition abrogates colorectal cancer stemness. Nat Commun. 2016 Aug 26;7:12586. [Content Brief]

[2]. Sugano T, et al., Pharmacological blockage of transforming growth factor-β signalling by a Traf2- and Nck-interacting kinase inhibitor, NCB-0846. Br J Cancer. 2021 Jan;124(1):228-236. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6637 mL	13.3184 mL	26.6368 mL	66.5921 mL
	5 mM	0.5327 mL	2.6637 mL	5.3274 mL	13.3184 mL
	10 mM	0.2664 mL	1.3318 mL	2.6637 mL	6.6592 mL
	15 mM	0.1776 mL	0.8879 mL	1.7758 mL	4.4395 mL
	20 mM	0.1332 mL	0.6659 mL	1.3318 mL	3.3296 mL
	25 mM	0.1065 mL	0.5327 mL	1.0655 mL	2.6637 mL
	30 mM	0.0888 mL	0.4439 mL	0.8879 mL	2.2197 mL
	40 mM	0.0666 mL	0.3330 mL	0.6659 mL	1.6648 mL
	50 mM	0.0533 mL	0.2664 mL	0.5327 mL	1.3318 mL
	60 mM	0.0444 mL	0.2220 mL	0.4439 mL	1.1099 mL

Keywords

NCB-0846

4 Cited Publications

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NCB-0846

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Extracellular Vesicles (EVs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) NCB-0846

Alle Wnt Isoform-spezifische Produkte anzeigen

Alle MAP4K Isoform-spezifische Produkte anzeigen

Alle TGF-beta/Smad Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NCB-0846 Related Classifications

Art. -Nr.: HY-100830