CRISPR/Cas9
抑制剂选择性比较
CRISPR/Cas9产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S0102New |
L 189L 189 是一种新型的 human DNA ligase 的抑制剂,对于hLigI、hLigIII和hLigIV的IC50值分别为5μM、9μM和5μM。L 189 可抑制碱基切除修复(BER)和非同源末端连接(NHEJ)。L 189 可使癌细胞对DNA损伤特别敏感。 |
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S8844 |
BRD0539BRD0539 是一种有效的 Streptococcus pyogenes Cas9 (SpCas9) 的抑制剂,在体外DNA裂解试验中IC50值为22 μM。 |
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S2638 |
NU7441 (KU-57788)NU7441 (KU-57788)是一种高度有效的,选择性DNA-PK抑制剂,在无细胞试验中IC50为14 nM,也会抑制 mTOR 和 PI3K,对应的IC50值分别为1.7 μM和5 μM。它可降低NHEJ的频率,而增强Cas9介导DNA剪接后发生的同源重组修复率。 |
![]() ![]() Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6, fibrillarin, and tubulin were used as loading controls.Effects of DNAPK inhibitors on its autophosphorylation in bleomycin-treated cells.
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S7046 |
Brefeldin ABrefeldin A 作用于HCT 116细胞,抑制内酯抗生素和ATPase,作用于protein transport(蛋白转运),IC50为0.2 μM,诱导癌细胞分化和凋亡。它还能提高同源重组修复效率,是CRISPR-mediated HDR的增强剂。Brefeldin A 也是自噬和线粒体自噬的抑制剂。 |
![]() ![]() Cells were treated with brefeldin A or manumycin A, and the resulting supernatant was collected after 48 h for exosomal preparation (lanes 1 and 2), or exosomes obtained from C81 cells were trypsin-treated or freeze/thawed (F/T) and then trypsin-treated (lanes 3 and 4). Lanes 5 and 6, input exosome controls from C81 or CEM cells, respectively. Resulting exosomes were assayed for the presence of Tax by Western blotting. |
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S2775 |
NocodazoleNocodazole (Oncodazole)是一种微管聚合的快速可逆抑制剂,也抑制Abl、Abl(E255K)和Abl(T315I),对应的IC50值分别为0.21 μM,0.53 μM和0.64 μM。Nocodazole可提高CRISPR介导的同源重组效率,对增强精确的基因编辑效力具有加成作用。Nocodazole可诱导凋亡。 |
![]() ![]() A, HeLa cells were treated with DMSO, Taxol (100 nM for 16 h), or Nocodazole (Noco, 100 ng/ml for 16 h). Total cell lysates were probed with the indicated antibodies against Hippo components on Phos-tag SDS-polyacrylamide gels. O and * mark the non-phosphorylated and phosphorylated proteins, respectively. |
|
S7974 |
L755507L-755,507是一种有效的、选择性的β3肾上腺素能受体部分激动剂,EC50为0.43 nM。它能在iPSCs和其他细胞类型中增强CRISPR介导的同源重组修复效率。 |
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S8234 |
RS-1RS-1是刺激RAD51的化合物。能够增加RAD51的DNA结合活性。在体内外兔胚胎实验中,RS-1可增强Cas9和TALEN介导的基因敲入效率。 |
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S7827 |
4-Hydroxytamoxifen(Afimoxifene)4-Hydroxytamoxifen (Afimoxifene) 是tamoxifen的活性代谢产物,是一种选择性的雌激素受体调节分子,在乳腺癌的治疗和化学疗法中应用广泛。4-HT可激活intein-Cas9突变体的靶向修饰效率。 |
![]() ![]() CDK4/6 inhibitor resistance promotes diminished ER expression and activity. (a and b) Proliferation of MCF-7 and MR cells in the presence of different concentrations of ICI (a) or 4-hydroxytamoxifen (4-OHT) (b) was measured by the alamarBlue assay and plotted as % inhibition of proliferation against log concentration of inhibitor. Each data point represents the average value±s.d. of six replicates obtained in three independent experiments. |
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S7742 |
SCR7SCR7 是一种特异性 DNA Ligase IV 抑制剂,其阻断非同源性末端连接(NHEJ)。在哺乳动物细胞和小鼠胚胎中,SCR7可增加利用CRISPR/Cas9进行HDR介导的基因编辑效率,最高可增强至19倍。 |
![]() ![]() The start codon CUG of PTEN-long was mutated to AUG and PTENlong expression is significantly increased. gRNA1 and gRNA2 have similar efficiency in driving PTEN-long expression (lanes 1 and 2). Combined gRNA1 and gRNA2 (lane 3) did not enhance PTEN-long expression compared to lane 1 and 2. The ssODN is required for mutation of CTG to ATG through HDR and without which PTEN-long is not expressed (lane 4). PTEN-long cDNA cloned into pcDNA3.1 with CTG to ATG mutation was highly expressed in transfected HEK293T cells (lane 5). Lane 6 is protein ladder. Lanes 7–10 indicate that the combination of gRNA and ssODN is required to facilitate HDR occurrence and double-strand DNA break. |
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S2579 |
ZidovudineZidovudine (ZDV, Azidothymidine, NSC 602670)是一种逆转录酶抑制剂。它能够降低同源重组效率。Zidovudine降低了CRISPR介导的特定序列基因组敲入效率,但增强了其敲除效率。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S0102New |
L 189L 189 是一种新型的 human DNA ligase 的抑制剂,对于hLigI、hLigIII和hLigIV的IC50值分别为5μM、9μM和5μM。L 189 可抑制碱基切除修复(BER)和非同源末端连接(NHEJ)。L 189 可使癌细胞对DNA损伤特别敏感。 |
||
S8844 |
BRD0539BRD0539 是一种有效的 Streptococcus pyogenes Cas9 (SpCas9) 的抑制剂,在体外DNA裂解试验中IC50值为22 μM。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S2638 |
NU7441 (KU-57788)NU7441 (KU-57788)是一种高度有效的,选择性DNA-PK抑制剂,在无细胞试验中IC50为14 nM,也会抑制 mTOR 和 PI3K,对应的IC50值分别为1.7 μM和5 μM。它可降低NHEJ的频率,而增强Cas9介导DNA剪接后发生的同源重组修复率。 |
![]() ![]() Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6, fibrillarin, and tubulin were used as loading controls.Effects of DNAPK inhibitors on its autophosphorylation in bleomycin-treated cells.
|
|
S7046 |
Brefeldin ABrefeldin A 作用于HCT 116细胞,抑制内酯抗生素和ATPase,作用于protein transport(蛋白转运),IC50为0.2 μM,诱导癌细胞分化和凋亡。它还能提高同源重组修复效率,是CRISPR-mediated HDR的增强剂。Brefeldin A 也是自噬和线粒体自噬的抑制剂。 |
![]() ![]() Cells were treated with brefeldin A or manumycin A, and the resulting supernatant was collected after 48 h for exosomal preparation (lanes 1 and 2), or exosomes obtained from C81 cells were trypsin-treated or freeze/thawed (F/T) and then trypsin-treated (lanes 3 and 4). Lanes 5 and 6, input exosome controls from C81 or CEM cells, respectively. Resulting exosomes were assayed for the presence of Tax by Western blotting. |
|
S2775 |
NocodazoleNocodazole (Oncodazole)是一种微管聚合的快速可逆抑制剂,也抑制Abl、Abl(E255K)和Abl(T315I),对应的IC50值分别为0.21 μM,0.53 μM和0.64 μM。Nocodazole可提高CRISPR介导的同源重组效率,对增强精确的基因编辑效力具有加成作用。Nocodazole可诱导凋亡。 |
![]() ![]() A, HeLa cells were treated with DMSO, Taxol (100 nM for 16 h), or Nocodazole (Noco, 100 ng/ml for 16 h). Total cell lysates were probed with the indicated antibodies against Hippo components on Phos-tag SDS-polyacrylamide gels. O and * mark the non-phosphorylated and phosphorylated proteins, respectively. |
|
S7974 |
L755507L-755,507是一种有效的、选择性的β3肾上腺素能受体部分激动剂,EC50为0.43 nM。它能在iPSCs和其他细胞类型中增强CRISPR介导的同源重组修复效率。 |
||
S8234 |
RS-1RS-1是刺激RAD51的化合物。能够增加RAD51的DNA结合活性。在体内外兔胚胎实验中,RS-1可增强Cas9和TALEN介导的基因敲入效率。 |
||
S7827 |
4-Hydroxytamoxifen(Afimoxifene)4-Hydroxytamoxifen (Afimoxifene) 是tamoxifen的活性代谢产物,是一种选择性的雌激素受体调节分子,在乳腺癌的治疗和化学疗法中应用广泛。4-HT可激活intein-Cas9突变体的靶向修饰效率。 |
![]() ![]() CDK4/6 inhibitor resistance promotes diminished ER expression and activity. (a and b) Proliferation of MCF-7 and MR cells in the presence of different concentrations of ICI (a) or 4-hydroxytamoxifen (4-OHT) (b) was measured by the alamarBlue assay and plotted as % inhibition of proliferation against log concentration of inhibitor. Each data point represents the average value±s.d. of six replicates obtained in three independent experiments. |
|
S7742 |
SCR7SCR7 是一种特异性 DNA Ligase IV 抑制剂,其阻断非同源性末端连接(NHEJ)。在哺乳动物细胞和小鼠胚胎中,SCR7可增加利用CRISPR/Cas9进行HDR介导的基因编辑效率,最高可增强至19倍。 |
![]() ![]() The start codon CUG of PTEN-long was mutated to AUG and PTENlong expression is significantly increased. gRNA1 and gRNA2 have similar efficiency in driving PTEN-long expression (lanes 1 and 2). Combined gRNA1 and gRNA2 (lane 3) did not enhance PTEN-long expression compared to lane 1 and 2. The ssODN is required for mutation of CTG to ATG through HDR and without which PTEN-long is not expressed (lane 4). PTEN-long cDNA cloned into pcDNA3.1 with CTG to ATG mutation was highly expressed in transfected HEK293T cells (lane 5). Lane 6 is protein ladder. Lanes 7–10 indicate that the combination of gRNA and ssODN is required to facilitate HDR occurrence and double-strand DNA break. |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S2579 |
ZidovudineZidovudine (ZDV, Azidothymidine, NSC 602670)是一种逆转录酶抑制剂。它能够降低同源重组效率。Zidovudine降低了CRISPR介导的特定序列基因组敲入效率,但增强了其敲除效率。 |