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Cat. No.: HY-184592

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JAK1-IN-21

JAK1-IN-21, biotin-conjugated isoxazole derivative, is a JAK1 inhibitor. JAK1-IN-21 directly engages and stabilizes JAK1, reduces the phosphorylation of JAK1, STAT1 and AKT, induces apoptotic marker cleavage (PARP, Caspase-3, Caspase-7) and exhibits broad-spectrum antiproliferative activity against cancer cells. JAK1-IN-21 can be used for the study of liver cancer, prostate cancer, and breast cancer.

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

Formula: C₃₄H₃₄ClN₃O₅S
Molecular Weight:632.17

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

JAK1-IN-21 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

IC₅₀ & Target^[1]

JAK1

STAT1

Akt1

Caspase-3

Caspase-7

All JAK Isoforms :

All STAT Isoforms :

All Akt Isoforms :

All PARP Isoforms :

All Caspase Isoforms :

Cellular Effect

Cell Line	Type	Value	References
Mahlavu	IC50	2.73 μM	42395957
SNU-475	IC50	1.48 μM	42395957
LNCaP C4-2	IC50	0.89 μM	42395957
DU-145	IC50	1.39 μM	42395957
PC-3	IC50	1.41 μM	42395957
T47D	IC50	0.52 μM	42395957
MDA-MB-231	IC50	3.05 μM	42395957
MCF-10A	IC50	6.10 μM	42395957

In Vitro

JAK1-IN-21 (C160) (0.3-10 μM; 72 h) inhibits the proliferation of Mahlavu, SNU475, C4-2, DU145, PC3, T47D and MDA-MB-231 cells, with IC₅₀ values of 2.73, 1.48, 0.89, 1.39, 1.41, 0.52 and 3.05 μM, respectively^[1].
JAK1-IN-21 (1-5 μM; 24-48 h) causes pronounced inhibition of STAT1 phosphorylation and markedly reduces phosphorylated JAK1 levels in Mahlavu, DU145 and C4-2 cells^[1].
JAK1-IN-21 (10 μM; 30 min) results in a clear, dose-dependent protection of JAK1 from Pronase-mediated digestion^[1].
JAK1-IN-21 (5 μM; 1 h) increases the thermal stability of JAK1 in Mahlavu cell lysates in a CETSA assay^[1].
JAK1-IN-21 (1-5 μM; 24 h) induces robust cleavage of PARP, Caspase-3 and Caspase-7 in Mahlavu, DU145 and C4-2 cells^[1].
JAK1-IN-21 (120 min) exhibits great stability in human plasma retaining 89% of the parent compound^[1].
JAK1-IN-21 (0.3-10 μM; 3 days) suppresses C4-2 spheroid growth, resulting in smaller spheroid size, disrupted spheroid morphology and increased signs of apoptosis^[1].
JAK1-IN-21 (0.75-5 μM; 10 days) produces a pronounced antiproliferative effect in T47D spheroids^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

Mahlavu, SNU475, C4-2, DU145, PC3, T47D, MDA-MB-231 and MCF10A cells
Concentration:

0.3-10 μM
Incubation Time:

72 h
Result:

Inhibited the proliferation of T47D, C4-2, DU145, PC3, SNU475, Mahlavu, and MDA-MB-231 cells, with IC₅₀ values of 0.52, 0.89, 1.39, 1.41, 1.48, 2.73, and 3.05 μM, respectively.
Showed weaker inhibitory activity in MCF10A cells, with an IC₅₀ of 6.10 μM.

Western Blot Analysis^[1]

Cell Line:

Mahlavu, DU145, and C4-2 cells
Concentration:

1 μM, 5 μM
Incubation Time:

24 h, 48 h
Result:

Robustly inhibited the phosphorylation of JAK1 and STAT1, thereby suppressing JAK/STAT signaling.

Western Blot Analysis^[1]

Cell Line:

Mahlavu cell lysates
Concentration:

10 μM
Incubation Time:

30 min
Result:

Resulted in a clear, dose-dependent protection of JAK1 from Pronase-mediated digestion.

Western Blot Analysis^[1]

Cell Line:

Mahlavu cell lysates
Concentration:

5 μM
Incubation Time:

1 h
Result:

Increased the thermal stability of JAK1.
Consistently preserved higher levels of soluble JAK1 between 58 and 62 °C.

Western Blot Analysis^[1]

Cell Line:

Mahlavu, DU145 and C4-2 cells
Concentration:

1 μM, 5 μM
Incubation Time:

24 h
Result:

Induced robust cleavage of PARP, Caspase-3 and Caspase-7.
Exhibited significant apoptotic responses in Mahlavu and C4-2 cells even at low doses.

In Vivo

JAK1-IN-21 (C160) (2-50 μM; 72 h) does not cause lethality in wild-type zebrafish larvae, and the larvae displayed normal morphology with no signs of toxicity^[1].

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

Animal Model:

Wild-type zebrafish larvae at 2 dpf^[1]
Dosage:

2 μM, 5 μM, 10 μM or 10 μM, 30 μM, 50 μM
Administration:

72 h; daily medium renewal
Result:

Resulted in no morphological abnormalities or developmental defects at concentrations comparable to those used in cellular assays (2, 5, 10 μM).
Did not cause lethality at up to 50 μM.
Displayed normal morphology with no signs of toxicity even at 50 μM.

Chemical Information

Molecular Weight 632.17
Formula C₃₄H₃₄ClN₃O₅S
SMILES

O=C(OCC1=NOC(C2=CC=C(OCC3=CC=CC=C3C)C=C2)=C1C4=CC=C(Cl)C=C4)CCCCC5SCC(C5N6)NC6=O
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

Handling Instructions (2659 KB)

References

[1]. Ergüven M, et al. Biotinylated Diaryl Isoxazole Derivatives with Enhanced Janus Kinase 1 Inhibitory, Antiproliferative, and Apoptotic Activities in Cancer Cells. ACS Omega. 2026 Jun 17;11(25):36501-36519. [Content Brief]

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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.

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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JAK1-IN-21

All JAK Isoforms

All STAT Isoforms

All Akt Isoforms

All PARP Isoforms

All Caspase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

JAK1-IN-21 Related Classifications

HY-184592 Related Classifications