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  1. Apoptosis
  2. DAPK
  3. TNIK-IN-3

TNIK-IN-3 (化合物 21k) 是一種有效,選擇性和具有口服活性的 TNIK 抑制劑,IC50 值為 0.026 μM。TNIK-IN-3 還可以抑制 Flt4 (IC50=0.030 μM),Flt1 (IC50=0.191 μM) 和 DRAK1 (IC50=0.411 μM)。TNIK-IN-3 可用于結(jié)直腸癌的研究。

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TNIK-IN-3 Chemical Structure

TNIK-IN-3 Chemical Structure

CAS No. : 2754265-25-1

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10 mM * 1 mL in DMSO ¥2813
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1 mg ¥1300
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5 mg ¥3300
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10 mg ¥5200
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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

TNIK-IN-3 is a potent, selective and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK), with an IC50 of 0.026 μM. TNIK-IN-3 could also inhibit Flt4 (IC50=0.030 μM), Flt1 (IC50=0.191 μM) and DRAK1 (IC50=0.411 μM). TNIK-IN-3 can be used for the research of colorectal cancer[1].

IC50 & Target

IC50: 0.026 μM (TNIK)[1], 0.030 μM (Flt4)[1], 0.191 μM (Flt1)[1], 0.411 μM (DRAK1)[1]

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
DLD-1 IC50
8 μM
Compound: 21k
Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
[PMID: 34985886]
HCT-116 IC50
4.26 μM
Compound: 21k
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
[PMID: 34985886]
體外研究
(In Vitro)

TNIK-IN-3 (Compound 21k) 抑制 Aurora-A、GCK 和 MLK3,IC50 分別為 0.517 μM、3.657 μM 和 4.552 μM[1]。
TNIK-IN-3 (0.1-100 μM;3 天) 抑制 HCT116 和 DLD-1 細胞的活力,IC50 分別為 4.26 μM 和 8.00 μM[1]。
TNIK-IN-3 (2.5-40 μM;10 天) 劑量依賴性地抑制 HCT116 和 DLD-1 細胞的集落形成[1]。
TNIK-IN-3 (5-20 μM;48 h) 抑制 HCT116 和 DLD-1 細胞的遷移[1]。
TNIK-IN -3 (5-40 μM;48 h) 劑量依賴性抑制HCT116細胞中LRP5和LRP6蛋白、Wnt靶基因AXIN2和c-Myc的表達[1]。
TNIK- IN-3 (5-20 μM;48 h) 顯著抑制 Hela 細胞中 JNK1/2 的磷酸化[1]。

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

Cell Viability Assay[1]

Cell Line: HCT116 and DLD-1 cells
Concentration: 0.1-100 μM
Incubation Time: 3 days
Result: Inhibited cell viability in a dose-dependent manner.

Cell Viability Assay[1]

Cell Line: HCT116 cells
Concentration: 5, 10, 20, 40 μM
Incubation Time: 48 hours
Result: Inhibited the expression of Wnt target genes AXIN2 and c-Myc, LRP5 and LRP6 proteins.
體內(nèi)研究
(In Vivo)

TNIK-IN-3 (Compound 21k) (100-150 mg/kg;每天口服兩次,持續(xù) 18 天) 以劑量依賴性方式抑制腫瘤生長[1]。

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

Animal Model: Six-week-old female NOD-SCID mice were injected with HCT116 cells[1]
Dosage: 100, 150 mg/kg
Administration: P.o. twice daily for 18 days
Result: Significantly inhibited tumor growth at a dose of 150 mg/kg.
No obvious weight loss and no other side effects were observed.
分子量

387.41

Formula

C23H18FN3O2

CAS 號
性狀

固體

顏色

Off-white to light yellow

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 83.33 mg/mL (215.10 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5812 mL 12.9062 mL 25.8124 mL
5 mM 0.5162 mL 2.5812 mL 5.1625 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.88%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5812 mL 12.9062 mL 25.8124 mL 64.5311 mL
5 mM 0.5162 mL 2.5812 mL 5.1625 mL 12.9062 mL
10 mM 0.2581 mL 1.2906 mL 2.5812 mL 6.4531 mL
15 mM 0.1721 mL 0.8604 mL 1.7208 mL 4.3021 mL
20 mM 0.1291 mL 0.6453 mL 1.2906 mL 3.2266 mL
25 mM 0.1032 mL 0.5162 mL 1.0325 mL 2.5812 mL
30 mM 0.0860 mL 0.4302 mL 0.8604 mL 2.1510 mL
40 mM 0.0645 mL 0.3227 mL 0.6453 mL 1.6133 mL
50 mM 0.0516 mL 0.2581 mL 0.5162 mL 1.2906 mL
60 mM 0.0430 mL 0.2151 mL 0.4302 mL 1.0755 mL
80 mM 0.0323 mL 0.1613 mL 0.3227 mL 0.8066 mL
100 mM 0.0258 mL 0.1291 mL 0.2581 mL 0.6453 mL
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.

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Inquiry Information

產(chǎn)品名稱:
TNIK-IN-3
目錄號:
HY-145293
需求量: