CRISPR/Cas9

抑制剂选择性比较

CRISPR/Cas9产品

所有产品 CRISPR/Cas9激活剂(7) CRISPR/Cas9调节剂(1)

产品目录	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PI3K，IC50为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。	Cancer Cell, 2019, 36(2):179-193 FASEB J, 2019, 33(6):6778-6788 Mol Biol Rep, 2019, 10.1007/s11033-019-04605-0	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 A Brefeldin 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。	Cells, 2019, 8(3) Nanoscale, 2018, 10(18):8796-8805 Oncogene, 2018, 37(8):1107-1118	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	Nocodazole Nocodazole是一种微管聚合的快速可逆抑制剂，也抑制Abl， Abl(E255K)和Abl(T315I)，IC50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。	Nucleic Acids Res, 2019, 10.1093/nar/gkz602 Cancer Res, 2019, 10.1158/0008-5472 FEBS J, 2019, 286(5):963-974	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	L755507 L-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。	Hum Mutat, 2019, 10.1002/humu.23848
S8234	RS-1 RS-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 4-Hydroxytamoxifen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。	Cells, 2019, 8(6) J Cell Physiol, 2019, 10.1002/jcp.28910 Oncogene, 2017, 36(16):2255-2264	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	SCR7 SCR7 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。	Hum Mutat, 2019, 10.1002/humu.23848 Dev Cell, 2018, 45(4):526-536 J Biol Chem, 2018, 10.1074/jbc.RA118.006046	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.
S2579	Zidovudine Zidovudine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。	PLoS One, 2018, 13(3):e0194611

产品目录	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PI3K，IC50为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。	Cancer Cell, 2019, 36(2):179-193 FASEB J, 2019, 33(6):6778-6788 Mol Biol Rep, 2019, 10.1007/s11033-019-04605-0	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 A Brefeldin 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。	Cells, 2019, 8(3) Nanoscale, 2018, 10(18):8796-8805 Oncogene, 2018, 37(8):1107-1118	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	Nocodazole Nocodazole是一种微管聚合的快速可逆抑制剂，也抑制Abl， Abl(E255K)和Abl(T315I)，IC50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。	Nucleic Acids Res, 2019, 10.1093/nar/gkz602 Cancer Res, 2019, 10.1158/0008-5472 FEBS J, 2019, 286(5):963-974	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	L755507 L-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。	Hum Mutat, 2019, 10.1002/humu.23848
S8234	RS-1 RS-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 4-Hydroxytamoxifen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。	Cells, 2019, 8(6) J Cell Physiol, 2019, 10.1002/jcp.28910 Oncogene, 2017, 36(16):2255-2264	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	SCR7 SCR7 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。	Hum Mutat, 2019, 10.1002/humu.23848 Dev Cell, 2018, 45(4):526-536 J Biol Chem, 2018, 10.1074/jbc.RA118.006046	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.

产品目录

产品描述

文献引用

实验数据

S2579

Zidovudine

Zidovudine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。

PLoS One, 2018, 13(3):e0194611

Tags: CRISPR/Cas9 enhancer|CRISPR/Cas9 activator|CRISPR/Cas9 inhibitor