Cat. No.: HY-156816

ON 108600

(Synonyms: 108600)

Customer Review

Based on 1 Customer Validation

ON 108600 (108600) is a CK2 (CK2α1: IC₅₀ = 50 nM; CK2α2 = 5 nM), TNIK (IC₅₀= 5 nM) and DYRK (DYRK1A: IC₅₀ = 16 nM; DYRK1B = 7 nM; DYRK2: = 28 nM). ON 108600 suppresses the growth of CD44high/CD24low breast cancer stem cell (BCSC) populations, induces G2/M arrest and apoptosis in triple negative breast cancer (TNBC) cells, and inhibits tubulin polymerization. ON 108600 can be used for the study of chemotherapy-resistant and metastatic TNBC[1][2].

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

Purity: 98.65%
CAS No.: 1585246-23-6
Formula: C₂₂H₁₄Cl₂N₂O₆S₂
Molecular Weight:537.39

Storage:

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

ON 108600 Chemical Structure

CAS No.: 1585246-23-6

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

DYRK2

0.028 μM (IC₅₀)

DYRK1A

0.016 μM (IC₅₀)

DYRK1B

0.007 μM (IC₅₀)

CK2α2

0.005 μM (IC₅₀)

CK2α1

0.05 μM (IC₅₀)

All Casein Kinase Isoforms :

All DYRK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-22	IC₅₀	1 μM Compound: 29; 108600	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	36876904
MCF-10A	GI₅₀	2.5 μM	Shows little or no toxicity against MCF-10A. Shows little or no toxicity against MCF-10A.	34344863
MDA-MB-231	GI₅₀	0.12 μM	Inhibits the viability of MDA-MB-231. Inhibits the viability of MDA-MB-231.	34344863
MDA-MB-157	GI₅₀	0.18 μM	Inhibits the viability of MDA-MB-157. Inhibits the viability of MDA-MB-157.	34344863
MDA-MB-436	GI₅₀	0.2 μM	Inhibits the viability of MDA-MB-436. Inhibits the viability of MDA-MB-436.	34344863
MDA-MB-468	GI₅₀	0.2 μM	Inhibits the viability of MDA-MB-468. Inhibits the viability of MDA-MB-468.	34344863
MDA-MB-453	GI₅₀	0.75 μM	Inhibits the viability of MDA-MB-453. Inhibits the viability of MDA-MB-453.	34344863
BT-20	GI₅₀	0.25 μM	Inhibits the viability of BT-20. Inhibits the viability of BT-20.	34344863
Hs-578T	GI₅₀	0.15 μM	Inhibits the viability of Hs-587T. Inhibits the viability of Hs-587T.	34344863
HCC1806	GI₅₀	0.15 μM	Inhibits the viability of HCC1806. Inhibits the viability of HCC1806.	34344863
MCF7	GI₅₀	0.5 μM	Inhibits the viability of MCF7. Inhibits the viability of MCF7.	34344863
BT-474	GI₅₀	0.19 μM	Inhibits the viability of BT-474. Inhibits the viability of BT-474.	34344863
PBMC	GI₅₀	> 10 μM	Inhibits the viability of PBMC. Inhibits the viability of PBMC.	34344863

In Vitro

ON 108600 (108600) (24-72 h) inhibits the viability of TNBC cell lines MDA-MB-231, MDA-MB-468, Hs578T and BT-20, with GI₅₀ values of 0.1-0.2 μM, and shows little or no toxicity against normal cells including MCF-10A, NBSC-1, NBSC-2, PBMC, HFL and hMSC-TERT (GI₅₀ > 2.5 μM)^[1].
ON 108600 (0.1-3 μM; 24 h) inhibits phosphorylation of CK2α substrate AKT1 (Ser129), DYRK1A substrates CYCLIN D1 (Thr286) and p27 (Ser10), and TNIK substrate AXIN2 in MDA-MB-231 and Hs578T cells^[1].
ON 108600 (10-1000 nM; 72 h) suppresses colony and mammosphere formation of CD44high/CD24low BCSC populations purified from MDA-MB-231 and Hs578T cells^[1].
ON 108600 exhibits inhibition against recombinant CK2α1, CK2α2, TNIK, DYRK1A, DYRK1B and DYRK2 kinases^[1].
ON 108600 (72 h) induces G2/M arrest and apoptosis in MDA-MB-231 cells and CTG1883 TNBC organoids^[1].
ON 108600 (1 μM; 12 h) induces abnormal mitotic spindle formation with multipolar spindles and multiple centrosomes in HeLa cells^[1].
ON 108600 (72 h) inhibits growth and colony formation of Paclitaxel (HY-B0015)-resistant MDA-MB-231 and BT-20 cells (MDA-MB-231-TR and BT-20-TR) with the same efficiency as parental paclitaxel-sensitive cells^[1].
ON 108600 (2.5 and 5 μM; 48 h) inhibits cell viability, induces G0/G1 arrest and apoptosis in metastatic canine mammary gland tumor (CMGT) cells^[2].

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

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-231 (CD44high/CD24low), Hs578T (CD44high/CD24low)
Concentration:

10, 100, 250, 500, 1000 nM
Incubation Time:

72 h
Result:

Suppressed colony formation in a dose-dependent manner.
Suppressed mammosphere formation in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231, Hs578T
Concentration:

0.1, 0.5, 1.0, 1.5, 3.0 μM
Incubation Time:

24 h
Result:

Inhibited phosphorylation of AKT1 (Ser129), CYCLIN D1 (Thr286) and p27 (Ser10).
Reduced AXIN2 expression in a dose-dependent manner.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-231, CTG1883 organoids
Concentration:

0.125, 0.25, 0.5 μM
Incubation Time:

24, 48, 72 h
Result:

Induced G2/M arrest and increased sub-G1 fraction.

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-231, CTG1883 organoids
Concentration:

0.25, 0.5, 1.0, 1.5, 3.0 μM
Incubation Time:

24,48 h
Result:

Induced PARP and Caspase 3 cleavage in a dose-dependent manner.

Immunofluorescence^[1]

Cell Line:

HeLa
Concentration:

1 μM
Incubation Time:

12 h
Result:

Induced abnormal mitotic spindle formation with multipolar spindles and multiple centrosomes.

Cell Viability Assay^[2]

Cell Line:

Canine mammary gland tumor (CMGT) cells
Concentration:

1, 2, 2.5, 3, 4, 5 μM
Incubation Time:

24, 48 h
Result:

Inhibited cell viability in a dose- and time-dependent manner, with approximately 50% reduction at 2.5-5 μM for 48 h.

Apoptosis Analysis^[2]

Cell Line:

Canine mammary gland tumor (CMGT) cells
Concentration:

2.5, 5 μM
Incubation Time:

48 h
Result:

Increased late apoptotic cells from 2.65% to 29.65% and 48.50%, respectively.

Cell Cycle Analysis^[2]

Cell Line:

Canine mammary gland tumor (CMGT) cells
Concentration:

2.5, 5 μM
Incubation Time:

48 h
Result:

Induced G0/G1 arrest and increased G0/G1 population from 61.6% to 65.2% and 73.7%, respectively.

Immunofluorescence^[2]

Cell Line:

Canine mammary gland tumor (CMGT) cells
Concentration:

2.5, 5 μM
Incubation Time:

48 h
Result:

Induced nuclear damage.

In Vivo

ON 108600 (108600) (100 mg/kg; i.p.; every other day for 5 days) inhibits phosphorylation of CK2α and DYRK1A substrates (pAKT1 Ser129, pCYCLIN D1 Thr286) and reduces C-MYC expression in CTG1883 PDX tumor grafts in NSG mice^[1].
ON 108600 (50 or 100 mg/kg; i.p.; every other day for 21 days) inhibits tumor growth in MDA-MB-231 xenograft model in nude mice, without observable toxicity^[1].
ON 108600 (100 mg/kg; i.p.; every other day for 21 days) suppresses tumor growth in TM00098 (Paclitaxel (HY-B0015)-sensitive TNBC PDX) model in NSG mice, without adverse effects on body weight^[1].
ON 108600 (100 mg/kg; i.p.; every other day for 12-24 days) in combination with Paclitaxel synergistically suppresses tumor growth in chemotherapy-resistant TNBC PDX models (CTG1883 and CTG2397)^[1].
ON 108600 (100 mg/kg; i.p.; every other day for 14 days) in combination with Paclitaxel (HY-B0015) suppresses growth of pre-established lung metastases in the MDA-MB-231/LM2-4/mCherry metastatic model in NSG mice^[1].

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

Animal Model:

CTG1883 PDX tumor-bearing female NSG mice (8-12 weeks old)^[1]
Dosage:

100 mg/kg
Administration:

i.p.; every other day for 5 days
Result:

Inhibited phosphorylation of pAKT1 Ser129 and pCYCLIN D1 Thr286.
Reduced C-MYC expression in tumors.

Animal Model:

MDA-MB-231 xenograft-bearing female athymic nude mice (8-12 weeks old)^[1]
Dosage:

50, 100 mg/kg
Administration:

i.p.; every other day for 21 days
Result:

Inhibited tumor growth in a dose-dependent manner, with no observable toxicity or body weight loss.

Animal Model:

TM00098 PDX tumor-bearing female NSG mice (8-12 weeks old)^[1]
Dosage:

100 mg/kg
Administration:

i.p.; every other day for 21 days
Result:

Suppressed tumor growth without adverse effects on body weight.

Animal Model:

CTG1883 and CTG2397 PDX tumor-bearing female NSG mice (8-12 weeks old)^[1]
Dosage:

100 mg/kg
Administration:

i.p.; every other day for 12-24 days
Result:

Suppressed tumor growth.

Animal Model:

MDA-MB-231/LM2-4/mCherry metastatic model (lung metastases) in female NSG mice (7 weeks old)^[1]
Dosage:

100 mg/kg
Administration:

i.p.; every other day for 14 days
Result:

Suppressed growth of pre-established lung metastases.

Chemical Information

CAS No. 1585246-23-6
Appearance Solid
Molecular Weight 537.39
Formula C₂₂H₁₄Cl₂N₂O₆S₂
Color Brown to reddish brown
SMILES

ClC(C=CC=C1Cl)=C1CS(=O)(C2=CC=C(S/C(C(N3)=O)=C\C4=CC([N+]([O-])=O)=C(C=C4)O)C3=C2)=O
Synonyms

108600
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (186.08 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

1.8608 mL

9.3042 mL

18.6085 mL

5 mM

0.3722 mL

1.8608 mL

3.7217 mL

10 mM

0.1861 mL

0.9304 mL

1.8608 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (293 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

References

[1]. Sato K, et al. Simultaneous CK2/TNIK/DYRK1 inhibition by 108600 suppresses triple negative breast cancer stem cells and chemotherapy-resistant disease. Nat Commun. 2021 Aug 3;12(1):4671. [Content Brief]

[2]. Özkan A D, et al. Determination of the Apoptotic Effect of Raf2 and Nck-Interacting Protein Kinase Inhibitor on Metastatic Canine Mammary Gland Tumor Cells[J]. Online Turkish Journal of Health Sciences, 7(1): 117-122.

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8608 mL	9.3042 mL	18.6085 mL	46.5211 mL
	5 mM	0.3722 mL	1.8608 mL	3.7217 mL	9.3042 mL
	10 mM	0.1861 mL	0.9304 mL	1.8608 mL	4.6521 mL
	15 mM	0.1241 mL	0.6203 mL	1.2406 mL	3.1014 mL
	20 mM	0.0930 mL	0.4652 mL	0.9304 mL	2.3261 mL
	25 mM	0.0744 mL	0.3722 mL	0.7443 mL	1.8608 mL
	30 mM	0.0620 mL	0.3101 mL	0.6203 mL	1.5507 mL
	40 mM	0.0465 mL	0.2326 mL	0.4652 mL	1.1630 mL
	50 mM	0.0372 mL	0.1861 mL	0.3722 mL	0.9304 mL
	60 mM	0.0310 mL	0.1551 mL	0.3101 mL	0.7754 mL
	80 mM	0.0233 mL	0.1163 mL	0.2326 mL	0.5815 mL
	100 mM	0.0186 mL	0.0930 mL	0.1861 mL	0.4652 mL

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ON 108600

MCE Bioactive Compound Library

All Casein Kinase Isoforms

All DYRK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ON 108600 Related Classifications

HY-156816 Related Classifications