2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Cell Cycle/DNA Damage Apoptosis
  3. JAK HDAC Apoptosis
  4. JAK/HDAC-IN-2

JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers.

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

JAK/HDAC-IN-2 Chemical Structure

JAK/HDAC-IN-2 Chemical Structure

CAS No. : 3029138-43-7

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JAK/HDAC-IN-2 Related Antibodies

Top Publications Citing Use of Products

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JAK1 JAK2 JAK3 Tyk2 JAK

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers[1].

IC50 & Target[1]

JAK2

5.32 nM (IC50)

JAK1

27.15 nM (IC50)

JAK3

594.8 nM (IC50)

Tyk2

414.4 nM (IC50)

HDAC

170 nM (IC50)

HDAC1

340 nM (IC50)

HDAC2

303 nM (IC50)

HDAC3

58.7 nM (IC50)

HDAC6

4.44 nM (IC50)

HDAC10

116.1 nM (IC50)

HDAC11

724.4 nM (IC50)

HDAC4

>10000 nM (IC50)

HDAC5

>10000 nM (IC50)

HDAC7

>10000 nM (IC50)

HDAC8

>10000 nM (IC50)

HDAC9

>10000 nM (IC50)

In Vitro

JAK/HDAC-IN-2 (compound 21) exhibits great antiproliferative activities against K562, HL-60, and HEL cells (IC50=1.87, 2.26, and 0.33 μM, respectively). JAK/HDAC-IN-2 inhibits the proliferation of four solid tumor cells, MCF-7, HeLa, A549, and PC-3 (IC50=1.83, 2.88, 0.73, and 2.52 μM, respectively)[1].
JAK/HDAC-IN-2 (1, 5 μM; 24 h) possesses excellent proapoptotic activity in HEL cells and moderate proapoptotic activity in A549 cells[1].
JAK/HDAC-IN-2 (1, 5 μM; 24 h) significantly induces the inhibition of histone deacetylation and STAT3 phosphorylation in hematological malignancy HEL cells as well as solid tumor A549 cells by inhibiting both HDAC and JAK[1].

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

JAK/HDAC-IN-2 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HEL cells
Concentration: 1, 5 μM
Incubation Time: 24 h
Result: The apoptotic rates were 37.6% at 1 μM and 81.5% at 5 μM on HEL cells.

Western Blot Analysis[1]

Cell Line: A549 and HEL cells
Concentration: 1, 5 μM
Incubation Time: 24 h
Result: Bviously upgraded the expression level of acetyl-H3 and acetyl-tubulin in A549 cells in a dose-dependent manner.
Reduced the expression level of p-STAT3-Tyr705.
In Vivo

JAK/HDAC-IN-2 (compound 21; 50 mg/kg; Intraperitoneally; once a day for 18 consecutive days) exhibits effective antitumor activity in vivo against hematological malignancy HEL and solid tumors A549[1].
Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats[1].

IV (3 mg/kg) PO (15 mg/kg)
Tmax (h) 2.912
Cmax (ng/mL) 93.328
AUC0-t (ng/mL∗h) 656.241 745.249
t1/2 (h) 0.128 2.084
CL (L/ kg∗h) 4.571 4.56
Vss (L/kg) 0.845
F (%) 22.71%

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

Animal Model: C57BL/6 nude mice[1]
Dosage: 50 mg/kg
Administration: Intraperitoneally; once a day for 18 consecutive days
Result: Prominently reduced the weight and volume of HEL and A549 xenografts.
Upgraded the expression level of acetyl-H3 as well as acetyl-tubulin and reduced the expression level of p-STAT3-Tyr705 in HEL as well as A549 xenograft tumor tissues.
Molecular Weight

570.70

Formula

C28H38N6O5S
CAS No.
SMILES

CC(NS(C1=CC(NC2=NC(NC3=CC=C(C=C3)OCCCCCCC(NO)=O)=NC=C2C)=CC=C1)(=O)=O)(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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JAK/HDAC-IN-2 Related Classifications

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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.

Keywords:

JAK/HDAC-IN-23029138-43-7JAKHDACApoptosisJanus kinaseHistone deacetylases2-amino-4-phenylaminopyrimidineJAK/HDACHDAC3HDAC6JAK1/2histone deacetylationSTAT3 phosphorylationhematological malignanciessolid cancersK562HL-60HELMCF-7HeLaA549PC-3Inhibitorinhibitorinhibit

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