Art. -Nr.: HY-146683

KS106

Name: KS106
Brand: MedChemExpress
SKU: HY-146683
Price: 300.00 USD
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KS106 is a potent ALDH inhibitor with IC₅₀s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase.

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Reinheit : 99.87%
CAS. Nr.: 2408477-50-7
Formel: C₁₈H₁₅BrF₃N₃O₂S
Molecular Weight:474.29

Speicherung:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

KS106 Chemical Structure

CAS. Nr.: 2408477-50-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (10)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

ALDH2

2137 nM (IC₅₀)

ALDH1A1

334 nM (IC₅₀)

ALDH3A1

360 nM (IC₅₀)

Alle Aldehyde Dehydrogenase (ALDH) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	5.7 μM Compound: 3h; KS106	Antiproliferative activity against human HCT116 cells measured after 72 hrs by MTS assay Antiproliferative activity against human HCT116 cells measured after 72 hrs by MTS assay	[PMID: 31887569]
HT-29	IC₅₀	4.9 μM Compound: 3h; KS106	Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTS assay Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTS assay	[PMID: 31887569]
MM1.S	IC₅₀	2.2 μM Compound: 3h; KS106	Antiproliferative activity against human MM.1S cells measured after 72 hrs by MTS assay Antiproliferative activity against human MM.1S cells measured after 72 hrs by MTS assay	[PMID: 31887569]
NCI-H929	IC₅₀	1.5 μM Compound: 3h; KS106	Antiproliferative activity against human NCIH929 cells measured after 72 hrs by MTS assay Antiproliferative activity against human NCIH929 cells measured after 72 hrs by MTS assay	[PMID: 31887569]
RPMI-8226	IC₅₀	1.6 μM Compound: 3h; KS106	Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay	[PMID: 31887569]
U-266	IC₅₀	2.6 μM Compound: 3h; KS106	Antiproliferative activity against human U266 cells measured after 72 hrs by MTS assay Antiproliferative activity against human U266 cells measured after 72 hrs by MTS assay	[PMID: 31887569]
UACC-903	IC₅₀	5.7 μM Compound: 3h; KS106	Antiproliferative activity against human UACC 903 cells measured after 72 hrs by MTS assay Antiproliferative activity against human UACC 903 cells measured after 72 hrs by MTS assay	[PMID: 31887569]

In Vitro

KS106 (compound 3h) (0-100 µM; 72 h) shows anti-proliferative activity with IC₅₀s of 5.7, 5.7, 5.7, 4.9, 1.5, 2.6, 1.6, 1.7, 2.2, 20.7 µM for UACC 903, 1205 Lu, HCT116, HT29, NCIH929, U266, RPMI8226, MM.1R, MM.1S, FF2441 cells, respectively^[1].
KS106 (5 µM, 24 h) induces apoptosis and cell cycle arrest at the G2/M phase^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Apoptosis Analysis^[1]

View Protocol

Cell Line:

HCT116, HT29 cells
Concentration:

5 µM
Incubation Time:

24 h
Result:

Induced cell apoptosis.

Cell Cycle Analysis^[1]

View Protocol

Cell Line:

HCT116 cells
Concentration:

5 µM
Incubation Time:

24 h
Result:

Induced cell cycle arrest at G2/M phase.

Chemical Information

CAS. Nr. 2408477-50-7
Appearance Solid
Molecular Weight 474.29
Formel C₁₈H₁₅BrF₃N₃O₂S
Color Light yellow to yellow
SMILES

N=C(SCC1=CC=C(C=C1)CN2C(C(C3=CC(C(F)(F)F)=CC=C32)=O)=O)N.Br
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (210.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.1084 mL

10.5421 mL

21.0841 mL

5 mM

0.4217 mL

2.1084 mL

4.2168 mL

10 mM

0.2108 mL

1.0542 mL

2.1084 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: ≥ 2.5 mg/mL (5.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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

All Cell Biology Signal Pathway Related

Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Dinavahi SS, et al. Design, synthesis characterization and biological evaluation of novel multi-isoform ALDH inhibitors as potential anticancer agents. Eur J Med Chem. 2020 Feb 1;187:111962. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1084 mL	10.5421 mL	21.0841 mL	52.7104 mL
	5 mM	0.4217 mL	2.1084 mL	4.2168 mL	10.5421 mL
	10 mM	0.2108 mL	1.0542 mL	2.1084 mL	5.2710 mL
	15 mM	0.1406 mL	0.7028 mL	1.4056 mL	3.5140 mL
	20 mM	0.1054 mL	0.5271 mL	1.0542 mL	2.6355 mL
	25 mM	0.0843 mL	0.4217 mL	0.8434 mL	2.1084 mL
	30 mM	0.0703 mL	0.3514 mL	0.7028 mL	1.7570 mL
	40 mM	0.0527 mL	0.2636 mL	0.5271 mL	1.3178 mL
	50 mM	0.0422 mL	0.2108 mL	0.4217 mL	1.0542 mL
	60 mM	0.0351 mL	0.1757 mL	0.3514 mL	0.8785 mL
	80 mM	0.0264 mL	0.1318 mL	0.2636 mL	0.6589 mL
	100 mM	0.0211 mL	0.1054 mL	0.2108 mL	0.5271 mL

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KS106

Alle Aldehyde Dehydrogenase (ALDH) Isoform-spezifische Produkte anzeigen