2. MAPK/ERK Pathway
  3. JNK
  4. JAK3-IN-13

JAK3-IN-13 是一种有效、选择性和口服活性的JAK3抑制剂，对 NK1、JNK2、JNK3、Tyk2 的 IC50 值分别为 4728、2039、8、365 nM。JAK3-IN-13 显示出抗增殖活性。JAK3-IN-13诱导细胞周期停滞在 G0/G1 期。JAK3-IN-13 具有抗肿瘤活性。

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JAK3-IN-13 Chemical Structure

JAK3-IN-13 Chemical Structure

CAS No. : 2803329-86-2

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JAK3-IN-13 相关抗体

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JNK1 JNK2 JNK3 JNK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JAK3-IN-13 is a potent, selective and orally active JAK3 inhibitor with IC50 values of 4728, 2039, 8, 365 nM for NK1, JNK2, JNK3, Tyk2, respectively. JAK3-IN-13 shows antiproliferative activity. JAK3-IN-13 induces cell cycle arrest at G0/G1 phase. JAK3-IN-13 shows antitumor activity[1].

IC50 & Target[1]

JNK1

4728 nM (IC50)

JNK2

2039 nM (IC50)

JNK3

8 nM (IC50)

Tyk2

365 nM (IC50)

体外研究
(In Vitro)

JAK3-IN-13 (compound 12n) (10 μM; 72 h) shows antiproliferative activity in BaF3-JAK3M511I, U937, parental cells[1].
JAK3-IN-13 inhibits the activity of TEL-JNK1, TEL-JNK2, JNK3M511I, JNK3 with IC50 values of 177.7, 134.2, 22.9, 1.2 nM, respectively[1].
JAK3-IN-13 inhibits (0-800 nM; 0-24 h) decreases the expression of phosphorylation JAK3, STAT3, and STAT5 in a dose-dependent manner[1].
JAK3-IN-13 inhibits (0-330 nM; 24 h) induces cell cycle arrest at G0/G1 phase and down-regulates the expression of cyclin-dependent kinase 2 (CDK2), CDK4, CDK6, cyclin B1, cyclin D3, and cyclin E1 in a concentration-dependent manner[1].

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

JAK3-IN-13 相关抗体:

Cell Proliferation Assay[1]

Cell Line: BaF3-JAK3M511I, U937, parental, COLO-205, H1299, HCT-116, MDA-MB-231, AGS, HL 7702 cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50s of 22.9, 20.2, 165.1 nM for BaF3-JAK3M511I, U937, parental cells, and >10, >10, >10, >10, >10, 3.27 μM for COLO-205, H1299, HCT-116, MDA-MB-231, AGS, HL 7702 cells, respectively.

Western Blot Analysis[1]

Cell Line: U937 cells
Concentration: 0-800 nM
Incubation Time: 0-24 h
Result: Dose-dependently suppressed the phosphorylation of JAK3, STAT3, and STAT5 and achieved near-complete inhibition at 200 nM.

Cell Cycle Analysis[1]

Cell Line: U937 cells
Concentration: 0-330 nM
Incubation Time: 24 h
Result: Induced cell cycle arrest at G0/G1 phase and down-regulated the expression of cyclin-dependent kinase 2 (CDK2), CDK4, CDK6, cyclin B1, cyclin D3, and cyclin E1 in a concentration-dependent manner.
体内研究
(In Vivo)

JAK3-IN-13 (5 mg/kg for i.v.; 15 mg/kg for p.o.) shows good PK properties and oral bioavailability of 20.66%[1].
JAK3-IN-13 (12.5, 25, 50 mg/kg; p.o.; twice daily for 10 days) shows antitumor activity and inhibits the expression of phosphorylation JAK3, STAT3, STAT5, CDK2, CDK4, CDK6, cyclin B1, cyclin D3, and cyclin E1[1]. Pharmacokinetic Parameters of JAK3-IN-13 in Male Sprague-Dawley rats[1].

12n i.v.(5 mg/kg) p.o.(15 mg/kg)
anminal no. 3 3
T1/2 (h) 0.91 0.98
Cmax (ng/mL) 911.33 238.28
AUC(0-∞) (h·ng/mL) 536.99 333.50
CL (mL/min/kg) 155.22
F % 20.66
Male Sprague-Dawley rats, 5 mg/kg iv (5% DMSO + 10% solutol + 85% saline); 15 mg/kg po (0.5% HPMC in water)[1]

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

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 5 mg/kg for i.v.; 15 mg/kg for p.o.
Administration: I.v. or p.o.
Result: Showed good PK properties and oral bioavailability of 20.66%.
Animal Model: Male CB17-SCID mice (U937 mouse xenograft model)[1]
Dosage: 12.5, 25, 50 mg/kg
Administration: P.o.; twice daily for 10 days (10 mg/kg; i.p.; once daily)
Result: Dose-dependently inhibited the growth of the U937 tumor and significantly inhibited the expression of phosphorylation JAK3, STAT3, and STAT5 as well as the cell cycle-related proteins.
分子量

533.02

Formula

C25H33ClN6O5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

JAK3-IN-13 相关分类

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  • 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:

JAK3-IN-132803329-86-2JNKc-Jun N-terminal kinaseantiproliferativeorally activephosphorylation JAK3STAT3STAT5G0/G1 phaseU937 cellsantitumor activityInhibitorinhibitorinhibit

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