| S7827 |
4-Hydroxytamoxifen (Afimoxifene)
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4-Hydroxytamoxifen (Afimoxifene) is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants.
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Signal Transduct Target Ther, 2025, 10(1):97
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Cell Death Differ, 2025, 10.1038/s41418-025-01514-7
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Proceedings of the National Academy of Sciences, 2025, e2421421122
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| S2638 |
NU7441 (KU-57788)
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NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM. It also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively, and reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.
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Nat Cell Biol, 2025, 27(1):59-72
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Trends Biotechnol, 2025, S0167-7799(25)00314-2
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Nat Commun, 2025, 16(1):997
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| S2775 |
Nocodazole
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Nocodazole is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.
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Adv Mater, 2025, e17493.
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Nat Commun, 2025, 16(1):7898
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EMBO J, 2025, 44(22):6556-6597
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| S8844 |
BRD0539
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BRD0539 is a potent inhibitor of Streptococcus pyogenes Cas9 (SpCas9) with IC50 of 22 μM in an in vitro DNA cleavage assay.
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Mol Cell, 2021, S1097-2765(21)00168-4
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| S7046 |
Brefeldin A (BFA chemical)
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Brefeldin A (BFA) is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells, induces cancer cell differentiation and apoptosis. It could also improve the HDR(homology-directed repair) efficiency and be an enhancer of CRISPR-mediated HDR. Brefeldin A is also an inhibitor of autophagy and mitophagy.
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Protein Cell, 2025, pwaf020
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Cancer Commun (Lond), 2025, 10.1002/cac2.70036
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J Integr Plant Biol, 2025, 67(8):2229-2244
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| S7742 |
SCR7
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SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ). It increases the efficiency of HDR-mediated genome editing up to 19-fold using CRISPR/Cas9 in mammalian cells and mouse embryos.
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Nucleic Acids Research, May 27, 2022, gkac448
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eLife, July 9, 2020, e56008
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Mol Ther, 2025, S1525-0016(25)00650-1
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| S2579 |
Zidovudine
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Zidovudine (ZDV, Azidothymidine, NSC 602670) is a nucleoside analogue reverse transcriptase inhibitor, used to treat HIV. This compound could decrease the HDR efficiency and decrease CRISPR-mediated sequence-specific genome knockin events while increaseing knockout efficiency.
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Biomolecules, August 6, 2025, 1132
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Scientific Reports, April 18, 2018, 6194
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Nat Commun, 2024, 15(1):2716
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| S7974 |
L755507
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L-755,507 is characterized as a potent and selective β3 adrenergic receptor partial agonist with EC50 of 0.43 nM. It is also recently identified to enhance CRISPR-mediated homology-directed repair (HDR) efficiency in human induced pluripotent stem cells (iPSCs) and other cell types.
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Human Mutation, November 15, 2019, 2044-2056
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Frontiers in Cell and Developmental Biology, January 25, 2024, 11:1276890
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Frontiers in Cell and Developmental Biology, January 25, 2024, 1276890
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| S8234 |
RS-1
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RS-1 is a RAD51-stimulatory compound, which increases the DNA binding activity of RAD51. It is an HDR(homology-directed repair) enhancer that enhances Cas9- and TALEN-mediated knock-in efficiency in rabbit embryos both in vitro and in vivo.
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Sci Bull (Beijing), 2025, S2095-9273(25)00865-5
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Functional & Integrative Genomics, 2025, 180
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Funct Integr Genomics, 2025, 25(1):180
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| S0102 |
L 189
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L 189 is a novel human DNA ligase inhibitor with IC50 of 5 μM, 9 μM and 5 μM for hLigI, hLigIII and hLigIV, respectively. This compound inhibits base excision repair (BER) and non-homologous end joining (NHEJ). It specifically sensitizes cancer cells to DNA damage.
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Research Square, May 2025, nan
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