2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK
  4. JAK2-IN-6

JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells.

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JAK2-IN-6 Chemical Structure

JAK2-IN-6 Chemical Structure

CAS No. : 353512-04-6

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Based on 1 publication(s) in Google Scholar

JAK2-IN-6 Related Antibodies

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Description

JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells[1].

IC50 & Target[1]

JAK2

22.86 μg/mL (IC50)

In Vitro

JAK2-IN-6 (Compound B2; 6.3-50 μg/mL; 48 hours; PC-9, H1975 and PANC-1 cells) treatment exhibits significantly antiproliferative activity against all of these cancer cell lines, with IC50 values of 18.1 μg/mL, 58.3 μg/mL, 40.6 μg/mL against PC-9, H1975 and PANC-1, respectively[1].
JAK2-IN-6 (Compound B2), an intramolecular hydrogen bond is formed, holding the chlorothiophene substituent coplanar with the aminothiazole core. The chlorothiophene moiety is found to be located in the binding pocket adjacent to Val863 and Leu983, and extends towards the Asp994 of activation loop and the Gly993 of glycine-rich loop[1].

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

JAK2-IN-6 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: PC-9, H1975 and PANC-1 cells
Concentration: 6.3 μg/mL, 12.5 μg/mL, 25 μg/mL, 50 μg/mL
Incubation Time: 48 hours
Result: Exhibited significantly antiproliferative activity against all of these cancer cell lines.
Molecular Weight

335.83

Formula

C14H10ClN3OS2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(N)N=C(NC2=CC=CC=C2)S1)C3=CC=C(Cl)S3
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 : 60 mg/mL (178.66 mM; ultrasonic and adjust pH to 5 with HCl; 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 2.9777 mL 14.8885 mL 29.7770 mL
5 mM 0.5955 mL 2.9777 mL 5.9554 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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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.14%

COA (250 KB) HNMR (259 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

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 2.9777 mL 14.8885 mL 29.7770 mL 74.4424 mL
5 mM 0.5955 mL 2.9777 mL 5.9554 mL 14.8885 mL
10 mM 0.2978 mL 1.4888 mL 2.9777 mL 7.4442 mL
15 mM 0.1985 mL 0.9926 mL 1.9851 mL 4.9628 mL
20 mM 0.1489 mL 0.7444 mL 1.4888 mL 3.7221 mL
25 mM 0.1191 mL 0.5955 mL 1.1911 mL 2.9777 mL
30 mM 0.0993 mL 0.4963 mL 0.9926 mL 2.4814 mL
40 mM 0.0744 mL 0.3722 mL 0.7444 mL 1.8611 mL
50 mM 0.0596 mL 0.2978 mL 0.5955 mL 1.4888 mL
60 mM 0.0496 mL 0.2481 mL 0.4963 mL 1.2407 mL
80 mM 0.0372 mL 0.1861 mL 0.3722 mL 0.9305 mL
100 mM 0.0298 mL 0.1489 mL 0.2978 mL 0.7444 mL
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JAK2-IN-6 Related Classifications

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.

Keywords:

JAK2-IN-6353512-04-6JAKJanus kinaseJAK2anti-canceranti-proliferativeglycine-richaminothiazoleInhibitorinhibitorinhibit

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