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Cat. No. | Product Name | Target | Signaling Pathways |
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T22461 |
YKL-5-124
|
CDK | Cell Cycle/Checkpoint |
YKL-5-124 是选择性不可逆CDK7共价抑制剂,对CDK7和CDK7/Mat1/CycH 的IC50分别为 53.5 nM 和 9.7 nM。它诱导强烈的细胞周期停滞,并抑制 E2F 驱动的基因表达。它对 CDK7 的生化和细胞选择性优于 CDK12/13。它对CDK7的选择性比 CDK9 和 CDK2 高 100 倍以上。 | |||
T16868 |
SEC inhibitor KL-2
KL-2 |
Others | Others |
SEC inhibitor KL-2 (KL-2) (KL-2) 是一种拟肽先导化合物,有效的选择性 SEC 抑制剂,通过破坏 SEC 支架蛋白 AFF4 和 P-TEFb 之间的相互作用,导致 Pol II 从启动子近端暂停位点的释放受损并且进行性转录延伸的平均速率降低。SEC inhibitor KL-2 剂量依赖性地抑制 AFF4-CCNT1 相互作用,Ki 值为 1.50 μM。 | |||
T16867 |
SEC inhibitor KL-1
KL-1 |
Others | Others |
SEC inhibitor KL-1 (KL-1) 是一种拟肽先导化合物,是一种有效的选择性SEC 抑制剂,能够剂量依赖性地抑制 AFF4-CCNT1 相互作用。它能够破坏 SEC 支架蛋白 AFF4 和 P-TEFb 之间的相互作用,导致 Pol II 从启动子近端暂停位点的释放受损,并且进行性转录延伸的平均速率降低。 | |||
T64150 | CX-5461 dihydrochloride | ||
CX-5461 dihydrochloride 是一种有效的、口服具有活力的 Pol I 介导的 rRNA synthesis 抑制剂,能够作用于 HCT-116 细胞 (IC50: 142 nM),A375 细胞 (IC50: 113 nM) 和 MIA PaCa-2 细胞 (IC50: 54 nM),对 Pol II 作用较小 (IC50≥25 μM)。 | |||
T74630 |
RNA polymerase II-IN-1
|
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
RNA polymerase II-IN-1(compound 19iv)是一款鹅膏毒素类化合物,能够抑制RNA聚合酶II(Pol II),其半抑制浓度IC50为36.66 nM。该化合物相较于α-Amanitin,对癌细胞展现出更高的细胞毒性,而对正常细胞的毒性较低。 | |||
T74631 |
RNA polymerase II-IN-2
|
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RNA polymerase II-IN-2 (compound 20iii)是高效的RNA polymerase II (Pol II)抑制剂,其Ki值为74.1 nM。该化合物对癌细胞展现出细胞毒性,其对CHO和HEK293细胞的毒性分别为α-amanitin的2倍和5倍。 | |||
T69908 |
Pidnarulex HCl
|
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Pidnarulex HCl is the salt form of CX-5461, a first-in-class non-genotoxic small molecule targeted inhibitor of RNA polymerase I (Pol I) that activates the p53 pathway without causing DNA damage. CX-5461 selectively inhibits rRNA synthesis by Pol I in the nucleolus, but does not inhibit mRNA synthesis by RNA Polymerase II (Pol II) and does not inhibit DNA replication or protein synthesis. Inhibition of Pol I results in nucleolar stress and release of ribosomal proteins (RP) from the nucleolus. T... | |||
T69931 |
MFH290
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MFH290 is a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation ... | |||
T82758 |
CDK9-Cyclin T1 PPI-IN-1
|
CDK | Cell Cycle/Checkpoint |
CDK9-Cyclin T1 PPI-IN-1 (Compound B19) 是CDK9-Cyclin T1蛋白-蛋白相互作用的选择性抑制剂。该化合物能够有效抑制TNBC MDA-MB-231细胞系的细胞增殖(IC50: 0.044 μM),诱导细胞凋亡,同时降低CDK9的转录活性并减少RNA Pol II CTD ser2的磷酸化,有效地抑制了4T1移植瘤模型小鼠中肿瘤的生长。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T17143 |
Toyocamycin
丰加霉素,Vengicide |
Apoptosis; Others; IRE1; Antibiotic; Antifungal | Apoptosis; Cell Cycle/Checkpoint; Microbiology/Virology; Others |
Toyocamycin (Vengicide) 是放线菌类产生的腺苷类似物,为 X 盒结合蛋白 1 (XBP1) 抑制剂,抑制 IRE1α 诱导的 ATP 依赖性 XBP1 mRNA 的断裂,IC50值为 80 nM。它还诱导凋亡。 |