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  2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. Molecular Glues CDK Apoptosis
  4. (R)?-?CR8

(R)?-?CR8 (CR8) 是 Roscovitine 的第二代類(lèi)似物，是一種有效的 CDK1/2/5/7/9 抑制劑。(R)?-?CR8 (CR8) 抑制 CDK1/cyclin B (IC50=0.09 μM)、CDK2/cyclin A (0.072 μM)、CDK2/cyclin E (0.041 μM)、CDK5/p25 (0.11 μM)、CDK7/cyclin H (1.1 μM)、CDK9/cyclin T (0.18 μM) 和 CK1δ/ε (0.4 μM)。(R)?-?CR8 (CR8) 誘導(dǎo)細(xì)胞凋亡并具有神經(jīng)保護(hù)作用。(R)?-?CR8 作為一種分子膠降解劑來(lái)消耗細(xì)胞周期蛋白 K。

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(R)?-?CR8 Chemical Structure

(R)?-?CR8 Chemical Structure

CAS No. : 294646-77-8

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥2750
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5 mg ￥2500
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10 mg ￥4000
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100 mg   詢價(jià)  

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Other Forms of (R)?-?CR8:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

(R)?-?CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)?-?CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)?-?CR8 induces apoptosis and has neuroprotective effect[1][2]. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K[3].

IC50 & Target[1]

Cdk1/cyclin B

0.09 μM (IC50)

cdk2/cyclin A

0.072 μM (IC50)

CDK2/cyclinE

0.041 μM (IC50)

Cdk5/p25

0.11 μM (IC50)

CDK7/cyclin H

1.1 μM (IC50)

CDK9/Cyclin T

0.18 μM (IC50)

CK1δ/ε

0.4 μM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
G-361 IC50
0.503 μM
Compound: CR8
Cytotoxicity against human G361 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay
Cytotoxicity against human G361 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay
[PMID: 26851505]
HCT-116 IC50
0.35 μM
Compound: CR8
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay
[PMID: 26851505]
HEK293 IC50
0.56 μM
Compound: 8m, (R)-C&R8
Antiproliferative activity against HEK293 cells assessed as survival after 48 hrs by MTS reduction assay
Antiproliferative activity against HEK293 cells assessed as survival after 48 hrs by MTS reduction assay
[PMID: 18698753]
HT GI50
0.263 μM
Compound: CR8
Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay
Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay
[PMID: 30943029]
K562 IC50
0.175 μM
Compound: CR8
Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay
Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay
[PMID: 26851505]
MCF7 IC50
0.16 μM
Compound: CR8
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay
[PMID: 26851505]
Sf9 IC50
0.062 μM
Compound: CR8
Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP
Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP
[PMID: 30943029]
Sf9 IC50
0.062 μM
Compound: CR8
Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP
Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP
[PMID: 26851505]
Sf9 IC50
0.225 μM
Compound: CR8
Inhibition of recombinant human full-length N-terminal GST-His6 fused CDK5 (M1 to P292 residues)/N-terminal His6-tagged p25 (A104 to R307 residues) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [g
Inhibition of recombinant human full-length N-terminal GST-His6 fused CDK5 (M1 to P292 residues)/N-terminal His6-tagged p25 (A104 to R307 residues) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [g
[PMID: 30943029]
Sf9 IC50
0.272 μM
Compound: CR8
Inhibition of recombinant human N-terminal GST-His6-fused CDK9 (M1 to F372 residues)/N-terminal His6-tagged cyclin T1 (M1 to K726 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-3
Inhibition of recombinant human N-terminal GST-His6-fused CDK9 (M1 to F372 residues)/N-terminal His6-tagged cyclin T1 (M1 to K726 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-3
[PMID: 30943029]
Sf9 IC50
0.787 μM
Compound: CR8
Inhibition of His-tagged CDK1/Cyclin-B1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP
Inhibition of His-tagged CDK1/Cyclin-B1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP
[PMID: 30943029]
Sf9 IC50
1.769 μM
Compound: CR8
Inhibition of recombinant human N-terminal GST-His6-fused CDK7 (M1 to F346 residues)/N-terminal His-tagged cyclin H (M1 to L323 residues)/N-terminal His6-tagged MAT1 (M1 to S306 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2
Inhibition of recombinant human N-terminal GST-His6-fused CDK7 (M1 to F346 residues)/N-terminal His-tagged cyclin H (M1 to L323 residues)/N-terminal His6-tagged MAT1 (M1 to S306 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2
[PMID: 30943029]
Sf9 IC50
26.09 μM
Compound: CR8
Inhibition of recombinant human N-terminal GST-fused CDK4 (S4 to E303 residues)/cyclin D1 (Q4 to I295 residues) expressed in baculovirus infected Sf9 insect cells using RPPTLSPIPHIPR as substrate measured in presence of [gamma-33P]ATP
Inhibition of recombinant human N-terminal GST-fused CDK4 (S4 to E303 residues)/cyclin D1 (Q4 to I295 residues) expressed in baculovirus infected Sf9 insect cells using RPPTLSPIPHIPR as substrate measured in presence of [gamma-33P]ATP
[PMID: 30943029]
SH-SY5Y IC50
0.43 μM
Compound: 8m, (R)-C&R8
Antiproliferative activity against human SH-SY5Y cells assessed as survival after 48 hrs by MTS reduction assay
Antiproliferative activity against human SH-SY5Y cells assessed as survival after 48 hrs by MTS reduction assay
[PMID: 18698753]
體外研究
(In Vitro)

(R)-CR8 (CR8) (0.1-100 μM; 48 hours) is a potent inducer of apoptotic cell death with an IC50 of 0.49 μM for SH-SY5Y cell line[1].
(R)-CR8 (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage[1].
The CDK-bound form of (R)-CR8 has a solvent-exposed pyridyl moiety that induces the formation of a complex between CDK12-cyclin K and the CUL4 adaptor protein DDB1, bypassing the requirement for a substrate receptor and presenting cyclin K for ubiquitination and degradation[3].

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

Apoptosis Analysis[1]

Cell Line: SH-SY5Y cell line
Concentration: 0.1, 1, 10, 100 μM
Incubation Time: 24 hours
Result: Reduced cell survival in a dose-dependent manner.
體內(nèi)研究
(In Vivo)

(R)-CR8 (5?mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment[2].

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

Animal Model: Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330?g)[2]
Dosage: i.p.
Administration: 5?mg/Kg
Result: Resulted in a significant reduction in lesion size.
Clinical Trial
分子量

431.53

Formula

C24H29N7O
CAS 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)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(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 50 mg/mL (115.87 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.3173 mL 11.5867 mL 23.1734 mL
5 mM 0.4635 mL 2.3173 mL 4.6347 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?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(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.61%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?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 2.3173 mL 11.5867 mL 23.1734 mL 57.9334 mL
5 mM 0.4635 mL 2.3173 mL 4.6347 mL 11.5867 mL
10 mM 0.2317 mL 1.1587 mL 2.3173 mL 5.7933 mL
15 mM 0.1545 mL 0.7724 mL 1.5449 mL 3.8622 mL
20 mM 0.1159 mL 0.5793 mL 1.1587 mL 2.8967 mL
25 mM 0.0927 mL 0.4635 mL 0.9269 mL 2.3173 mL
30 mM 0.0772 mL 0.3862 mL 0.7724 mL 1.9311 mL
40 mM 0.0579 mL 0.2897 mL 0.5793 mL 1.4483 mL
50 mM 0.0463 mL 0.2317 mL 0.4635 mL 1.1587 mL
60 mM 0.0386 mL 0.1931 mL 0.3862 mL 0.9656 mL
80 mM 0.0290 mL 0.1448 mL 0.2897 mL 0.7242 mL
100 mM 0.0232 mL 0.1159 mL 0.2317 mL 0.5793 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(chēng)：
(R)?-?CR8
目錄號(hào)：
HY-18340
需求量：