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  2. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK Stem Cell/Wnt PI3K/Akt/mTOR
  3. CDK VEGFR GSK-3
  4. K00546

K00546 是一種有效的 CDK1 和 CDK2 抑制劑，對 CDK1/cyclin B 和 CDK2/cyclin A 的 IC50 分別為 0.6 nM 和 0.5 nM。K00546 也是一種有效的 CDC2 樣激酶 1 (CLK1) 和 CLK3 抑制劑，IC50 分別為 8.9 nM 和 29.2 nM。

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K00546 Chemical Structure

K00546 Chemical Structure

CAS No. : 443798-47-8

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥3080
In-stock
5 mg ￥2800
In-stock
10 mg ￥4500
In-stock
50 mg   詢價  
100 mg   詢價  

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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

K00546 is a potent CDK1 and CDK2 inhibitor with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50s of 8.9 nM and 29.2 nM, respectively[1][2][3].

IC50 & Target[1][2][3]

Cdk1/cyclin B

0.6 nM (IC50)

cdk2/cyclin A

0.5 nM (IC50)

CLK1

8.9 nM (IC50)

CLK3

29.2 nM (IC50)

VEGF-R2

32 nM (IC50)

GSK-3

140 nM (IC50)

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
Sf9 IC50
0.0002 μM
Compound: Fig.8B, R1C2
Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
[PMID: 30234987]
Sf9 IC50
0.002 μM
Compound: Fig.8B, R1C2
Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
[PMID: 30234987]
Sf9 IC50
0.003 μM
Compound: Fig.8B, R1C2
Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
[PMID: 30234987]
Sf9 IC50
0.03 μM
Compound: Fig.8B, R1C2
Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
[PMID: 30234987]
Sf9 IC50
0.059 μM
Compound: Fig.8B, R1C2
Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
[PMID: 30234987]
Sf9 IC50
0.066 μM
Compound: Fig.8B, R1C2
Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
[PMID: 30234987]
體外研究
(In Vitro)

K00546 與 SLK ATP 結(jié)合位點結(jié)合，與激酶鉸鏈殘基 E109 和 C111 形成三個氫鍵。K00546 的氨磺?；糠诌€與 L40 的主鏈相互作用[1]。
K00546 (化合物 3n) 還抑制 PKA、酪蛋白激酶-1、MAP 激酶 (ERK-2)、鈣調(diào)蛋白激酶、VEGF-R2、GSK-3 和 PDGF-Rβ，IC50 值分別為 5.2 μM、2.8 μM、1.0 μM、8.9 μM、0.032 μM、0.14 μM 和 1.6 μM[2]。

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

425.44

Formula

C15H13F2N7O2S2
CAS 號
性狀

固體

顏色

White to off-white

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 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 100 mg/mL (235.05 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 2.3505 mL 11.7525 mL 23.5051 mL
5 mM 0.4701 mL 2.3505 mL 4.7010 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，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(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

只
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
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，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(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 2.3505 mL 11.7525 mL 23.5051 mL 58.7627 mL
5 mM 0.4701 mL 2.3505 mL 4.7010 mL 11.7525 mL
10 mM 0.2351 mL 1.1753 mL 2.3505 mL 5.8763 mL
15 mM 0.1567 mL 0.7835 mL 1.5670 mL 3.9175 mL
20 mM 0.1175 mL 0.5876 mL 1.1753 mL 2.9381 mL
25 mM 0.0940 mL 0.4701 mL 0.9402 mL 2.3505 mL
30 mM 0.0784 mL 0.3918 mL 0.7835 mL 1.9588 mL
40 mM 0.0588 mL 0.2938 mL 0.5876 mL 1.4691 mL
50 mM 0.0470 mL 0.2351 mL 0.4701 mL 1.1753 mL
60 mM 0.0392 mL 0.1959 mL 0.3918 mL 0.9794 mL
80 mM 0.0294 mL 0.1469 mL 0.2938 mL 0.7345 mL
100 mM 0.0235 mL 0.1175 mL 0.2351 mL 0.5876 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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產(chǎn)品名稱：
K00546
目錄號：
HY-103647
需求量：