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  2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. CAY10603

CAY10603 (BML-281) 是一種有效的，選擇性的 HDAC6 抑制劑，IC50 值為 2 pM；CAY10603 (BML-281) 同時(shí)可抑制 HDAC1，HDAC2，HDAC3，HDAC8 和 HDAC10 的活性，IC50 值分別為 271，252，0.42，6851，90.7 nM。

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CAY10603 Chemical Structure

CAY10603 Chemical Structure

CAS No. : 1045792-66-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1081
In-stock
1 mg ￥440
In-stock
5 mg ￥1100
In-stock
10 mg ￥1800
In-stock
25 mg ￥3500
In-stock
50 mg ￥5500
In-stock
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor, with an IC50 of 2 pM; CAY10603 (BML-281) also inhibits HDAC1, HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 6851, 90.7 nM.

IC50 & Target[1]

HDAC6

0.002 nM (IC50)

HDAC3

0.42 nM (IC50)

HDAC10

90.7 nM (IC50)

HDAC2

252 nM (IC50)

HDAC1

271 nM (IC50)

HDAC8

6851 nM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 10 μM
Compound: CAY10603
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
[PMID: 35043615]
B16-F10 IC50
9.41 μM
Compound: CAY10603
Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
[PMID: 35043615]
BXPC-3 IC50
1 μM
Compound: 7
Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay
[PMID: 18642892]
HCT-116 IC50
1.47 μM
Compound: CAY10603
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
[PMID: 35043615]
HL-60 IC50
594 nM
Compound: CAY10603
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability for 72 hrs by Celltitre-Glo luminescent assay
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability for 72 hrs by Celltitre-Glo luminescent assay
[PMID: 33360560]
HMEC IC50
< 1 μM
Compound: 7
Cytotoxicity against HMEC after 72 hrs by MTT assay
Cytotoxicity against HMEC after 72 hrs by MTT assay
[PMID: 18642892]
HuP-T3 IC50
0.3 μM
Compound: 7
Antiproliferative activity against human HupT3 cells after 72 hrs by MTT assay
Antiproliferative activity against human HupT3 cells after 72 hrs by MTT assay
[PMID: 18642892]
Jurkat IC50
0.61 μM
Compound: CAY10603
Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 35043615]
MCF7 IC50
2.82 μM
Compound: CAY10603
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
[PMID: 35043615]
MIA PaCa-2 IC50
0.1 μM
Compound: 7
Antiproliferative activity against human MiaPaca2 cells after 72 hrs by MTT assay
Antiproliferative activity against human MiaPaca2 cells after 72 hrs by MTT assay
[PMID: 18642892]
Sf9 IC50
13.8 nM
Compound: 1b
Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by s
Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by s
[PMID: 31414801]
Sf9 IC50
3.2 nM
Compound: 1b
Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mi
Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mi
[PMID: 31414801]
SU.86.86 IC50
0.6 μM
Compound: 7
Antiproliferative activity against human SU.86.86 cells after 72 hrs by MTT assay
Antiproliferative activity against human SU.86.86 cells after 72 hrs by MTT assay
[PMID: 18642892]
體外研究
(In Vitro)

CAY10603（化合物7）對胰腺癌細(xì)胞系表現(xiàn)出強(qiáng)烈的抑制活性，針對BxPC-3、HupT3、Mia Paca-2、Panc 04.03、SU.86.86、HMEC、HPDE6c7細(xì)胞系的半數(shù)抑制濃度（IC50）分別為1、0.3、0.1、0.1、0.6、小于1、0.5 μM。此外，在100 nM至200-300 nM濃度下，CAY10603對Mia Paca-2和Panc04.03兩種細(xì)胞系均有效[1]。
CAY10603能夠抑制HDAC6脫乙酰酶的活性，并抑制肺腺癌細(xì)胞的增殖。它還能誘導(dǎo)肺腺癌細(xì)胞凋亡。進(jìn)一步研究表明，CAY10603與吉非替尼聯(lián)合使用可協(xié)同誘導(dǎo)肺腺癌細(xì)胞系的凋亡，部分機(jī)制是通過降低EGFR穩(wěn)定性及失活EGFR信號通路實(shí)現(xiàn)的[2]。

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

446.50

Formula

C22H30N4O6
CAS 號
性狀

固體

顏色

White to light yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 50 mg/mL (111.98 mM; 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)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.2396 mL 11.1982 mL 22.3964 mL
5 mM 0.4479 mL 2.2396 mL 4.4793 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(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)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

動物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.60 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.60 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請依序添加每種溶劑： 50% PEG300    50% Saline

    Solubility: 5 mg/mL (11.20 mM); 懸濁液; Need ultrasonic and warming and heat to 42°C

掃碼獲得
動物溶解方案

動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)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(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， PEG300/PEG400，Tween 80，均可在 MCE 網(wǎng)站選購。
純度 & 產(chǎn)品資料

純度: ≥98.0%

參考文獻(xiàn)
Kinase Assay
[1]

Purified HDACs are incubated with 1 mm carboxyfluorescein (FAM)-labeled acetylated peptide substrate and test compound for 17 h at 25°C in HDAC assay buffer containing 100 mm HEPES (pH 7.5), 25 mm KCl, 0.1% BSA, and 0.01% Triton X-100. Reactions are terminated by the addition of buffer containing 0.078% SDS for a final SDS concentration of 0.05%. Substrate and product are separated electrophoretically using a Caliper LabChip 3000 system with blue laser excitation and green fluorescence detection (CCD2). The fluorescence intensity in the substrate and product peaks is determined using the Well Analyzer software on the Caliper system. The reactions are performed in duplicate for each sample. IC50 values are automatically calculated using the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel and the XLFit 4-Parameter Logistic Model (sigmoidal dose-response model): ((A+ ((B_A)/1+((C/x)D)))), in which x is compound concentration, A and B are respectively the estimated minimum and maximum of percent inhibition, C is the inflection point, and D is the Hill slope of the sigmoidal curve.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

The pancreatic cancer cell lines BxPc-3, HupT3, Mia Paca-2, Panc 04.03, and SU 86.86 are obtained from ATCC and are grown in medium (DMEM or RPMI) containing 10% fetal calf serum and l-glutamine. Pancreatic cancer cells are plated out in duplicate into 6 wells of a 96-well microtiter plate at 2.5-4P103 cells per well. Four hours post plating, individual wells are treated with diluent (DMSO) or varying concentrations of SAHA or the indicated HDACIs from a concentration of 1 nm to 50 mm. Cytotoxicity is measured at time “0”, and 72 h post treatment using the colorimetric MTT assay. The IC50 values are calculated using XLfit.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

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(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲存時(shí)，請?jiān)?個(gè)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 2.2396 mL 11.1982 mL 22.3964 mL 55.9910 mL
5 mM 0.4479 mL 2.2396 mL 4.4793 mL 11.1982 mL
10 mM 0.2240 mL 1.1198 mL 2.2396 mL 5.5991 mL
15 mM 0.1493 mL 0.7465 mL 1.4931 mL 3.7327 mL
20 mM 0.1120 mL 0.5599 mL 1.1198 mL 2.7996 mL
25 mM 0.0896 mL 0.4479 mL 0.8959 mL 2.2396 mL
30 mM 0.0747 mL 0.3733 mL 0.7465 mL 1.8664 mL
40 mM 0.0560 mL 0.2800 mL 0.5599 mL 1.3998 mL
50 mM 0.0448 mL 0.2240 mL 0.4479 mL 1.1198 mL
60 mM 0.0373 mL 0.1866 mL 0.3733 mL 0.9332 mL
80 mM 0.0280 mL 0.1400 mL 0.2800 mL 0.6999 mL
100 mM 0.0224 mL 0.1120 mL 0.2240 mL 0.5599 mL

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產(chǎn)品名稱：
CAY10603
目錄號：
HY-18613
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