1. ABC1183

ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities.

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ABC1183 Chemical Structure

ABC1183 Chemical Structure

CAS No. : 1042735-18-1

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10 mM * 1 mL in DMSO
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Description

ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities[1].

In Vitro

ABC1183 (3 μM, 24 h) can block cell cycle progression and thus affect cell proliferation[1].

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

Cell Cycle Analysis[1]

Cell Line: LNCaP human prostate cancer cells
Concentration: 3 μM
Incubation Time: 24 hours
Result: Significantly reduced cells in the G1 and S phases and increased cells in the G2/M and sub-G1 cycle phases.
In Vivo

ABC1183 (oral gavage, 5 or 50 mg/kg) inhibits tumor proliferation through negative regulation of cell growth and pro-inflammatory signalling in male C57BL/6 mice[1].

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

Animal Model: Male C57BL/6 mice with melanoma B16[1]
Dosage: 5 mg/kg
Administration: Oral gavage; 5 times per week; 22 days
Result: Reduced tumor size and no observed toxicity.
Decreased the expression levels of GSK3 α /β, pSer21/9 and GS pSer641 but no change of total GS expression.
Animal Model: Male C57BL/6 mice infected crohn’s disease[1]
Dosage: 50 mg/kg
Administration: Oral gavage; everyday; 3 days
Result: Reduced TNF-α by 65%, IL-6 by 30% and IL-1β by 45%.
Animal Model: Male C57BL/6 mice with ulcerative colitis[1]
Dosage: 50 mg/kg
Administration: Oral gavage; once daily; 6 days
Result: Increased the expression of the anti-inflammatory factor IL-10, while decreasing the pro-inflammatory factor IL-6.
Molecular Weight

334.39

Formula

C18H14N4OS

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

N#CC1=CC=C(C(C2=C(N)N=C(NC3=CC=C(C)C=C3)S2)=O)C=C1

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 : 125 mg/mL (373.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9905 mL 14.9526 mL 29.9052 mL
5 mM 0.5981 mL 2.9905 mL 5.9810 mL
View the Complete Stock Solution Preparation Table

* 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.

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9905 mL 14.9526 mL 29.9052 mL 74.7630 mL
5 mM 0.5981 mL 2.9905 mL 5.9810 mL 14.9526 mL
10 mM 0.2991 mL 1.4953 mL 2.9905 mL 7.4763 mL
15 mM 0.1994 mL 0.9968 mL 1.9937 mL 4.9842 mL
20 mM 0.1495 mL 0.7476 mL 1.4953 mL 3.7381 mL
25 mM 0.1196 mL 0.5981 mL 1.1962 mL 2.9905 mL
30 mM 0.0997 mL 0.4984 mL 0.9968 mL 2.4921 mL
40 mM 0.0748 mL 0.3738 mL 0.7476 mL 1.8691 mL
50 mM 0.0598 mL 0.2991 mL 0.5981 mL 1.4953 mL
60 mM 0.0498 mL 0.2492 mL 0.4984 mL 1.2460 mL
80 mM 0.0374 mL 0.1869 mL 0.3738 mL 0.9345 mL
100 mM 0.0299 mL 0.1495 mL 0.2991 mL 0.7476 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    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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Product Name:
ABC1183
Cat. No.:
HY-100950
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