2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. JAK STAT Apoptosis
  4. JAK3-IN-20

JAK3-IN-20 是一种具有口服活性的选择性 JAK3 抑制剂，其 IC50 为 0.7473 nM。JAK3-IN-20 可与 JAK3 Cys909 形成共价键，竞争性占据 ATP 的催化位点结合区域，并阻断 JAK-STAT 通路的激活。JAK3-IN-20 可抑制对 Bortezomib (HY-10227) 耐药的癌细胞的迁移、增殖与肿瘤生长。JAK3-IN-20 可诱导剂量依赖性的细胞凋亡 (apoptosis)。JAK3-IN-20 可用于硼替佐米耐药性多发性骨髓瘤的相关研究。

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JAK3-IN-20

JAK3-IN-20 Chemical Structure

CAS No. : 3104109-31-8

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JAK3-IN-20 相关抗体

Top Publications Citing Use of Products

查看 JAK 亚型特异性产品:

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JAK1 JAK2 JAK3 Tyk2 JAK

查看 STAT 亚型特异性产品:

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STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JAK3-IN-20 is a selective and orally active JAK3 inhibitor with an IC50 of 0.7473 nM. JAK3-IN-20 forms a covalent bond with JAK3 Cys909, outcompetes ATP for catalytic site binding, and blocks JAK-STAT pathway activation. JAK3-IN-20 inhibits migration, proliferation, and tumor growth of Bortezomib (HY-10227)-resistant cancer cells. JAK3-IN-20 induces dose-dependent apoptosis. JAK3-IN-20 can be used for the research of Bortezomib-resistant multiple myeloma[1].

IC50 & Target[1]

JAK3

0.7473 nM (IC50)

体外研究
(In Vitro)

JAK3-IN-20 (Compound 7n) (60 min) 可强效抑制纯化的 JAK3 蛋白，其 IC50 为 0.7473 nM[1]。
JAK3-IN-20 (5 nM) 对 JAK3 具有高选择性，在 5 nM 时抑制率达 96.87%，对 JAK2 和 TYK2 仅表现出中等抑制作用，对 JAK1 无显著活性[1]。
JAK3-IN-20 (72 h) 可强效抑制 Bortezomib (HY-10227) 耐药型 KM3 多发性骨髓瘤细胞的增殖，其 IC50 为 0.245 μM；同时也能抑制 KM3、BaF3-JAK3、Raji、Paca-02、H1975、HK-2 和 LX-2 细胞的增殖，且 IC50 值在 0.211-4.317 μM 之间[1]。
JAK3-IN-20 (0.3125-5.0 μM; 48 h) 可在 Bortezomib 耐药的 KM3 多发性骨髓瘤细胞中诱导剂量依赖性凋亡并诱导 G2/M 期细胞阻滞[1]。
JAK3-IN-20 (78.13-312.5 nM; 48 h) 可浓度依赖性地抑制 Bortezomib 耐药的 KM3 多发性骨髓瘤细胞的迁移[1]。
JAK3-IN-20 (0.3125-5.0 μM; 48 h) 可在 Bortezomib 耐药的 KM3 多发性骨髓瘤细胞中以剂量依赖方式上调促凋亡蛋白 Bax，并下调抗凋亡蛋白 Bcl-2[1]。
JAK3-IN-20 (15.6 nM-4 μM; 1-72 h) 可剂量依赖性地抑制 Bortezomib 耐药的 KM3 多发性骨髓瘤细胞中 STAT5 的磷酸化[1]。

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

JAK3-IN-20 相关抗体:

Apoptosis Analysis[1]

Cell Line: Bortezomib-resistant KM3 multiple myeloma cells
Concentration: 0.3125, 1.25, 5.0 μM
Incubation Time: 48 h
Result: At 0.3125 μM, a small proportion of apoptotic cells (orange-stained nuclei) were observed.
At 1.25 μM, the proportion of apoptotic cells increased
At 5.0 μM, numerous advanced apoptotic cells with cracked nuclei were observed.
Confirmed chromatin condensation and nuclear disintegration across all tested concentrations via DAPI staining.

Western Blot Analysis[1]

Cell Line: Bortezomib-resistant KM3 multiple myeloma cells
Concentration: 15.6, 62.5, 250 nM, 1, 4 μM (24 h); 250 nM (1, 12, 24, 48, 72 h)
Incubation Time: 1, 12, 24, 48, 72 h
Result: At 250 nM, p-STAT5 expression decreased; inhibition increased in a dose-dependent manner, with further decreased p-STAT5 expression at 4 μM.
Showed maximal inhibition of p-STAT5 at 12 h, with gradual recovery of phosphorylation by 24 h in time-course analysis.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t AUC0-∞ MRT0-t MRT0-∞ Cmax F
Rat[1] 3 mg/kg i.v. 762.2 μg/L·h 785.5 μg/L·h 3.592 h 4.410 h 916.5 μg/L /
Rat[1] 30 mg/kg p.o. 3025 μg/L·h 3072 μg/L·h 7.478 h 7.812 h 306.8 μg/L 39.11 %
体内研究
(In Vivo)

JAK3-IN-20 (Compound 7n) (60 mg/kg；灌胃；每日一次；连续 21 天) 在 Bortezomib (HY-10227) 耐药的多发性骨髓瘤异种移植模型中展现出肿瘤生长抑制效果，且未出现显著的体重下降[1]。

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

Animal Model: NYG nude mice with KM3 cells (Bortezomib-
resistant) xenograft (~6 weeks old, ~20 g)[1]
Dosage: 60 mg/kg
Administration: p.o.; daily; 21 days
Result: Reduced tumor volume significantly lower than normal saline control and 60 mg/kg Tofacitinib (HY-40354) group on study day 21.
Caused no significant loss of body weight.
分子量

499.01

Formula

C24H31ClN8O2
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-20 相关分类

  • 摩尔计算器

  • 稀释计算器

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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-203104109-31-8JAKSTATApoptosisJanus kinaseATPbortezomib-resistant cancer cellsJAK-STAT pathwaySTAT5KM3 cellsmultiple myelomaJAK3Raji cellsCys909BaF3-JAK3 cellsInhibitorinhibitorinhibit

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