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Search Results for " polymerase-ii "

28

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8972	FIT-039	Others; DNA/RNA Synthesis; CDK; HSV	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others
	FIT-039 是一种选择性和 ATP 竞争性的口服活性 CDK9 抑制剂，对CKD9/cyclin T1的IC50为 5.8 μM。它抑制HSV-1(IC50为 0.69 μM)，HSV-2，人腺病毒和人CMV 的复制。它可抑制耐药性HSV 和其他 DNA 病毒，是有前途的抗病毒药物。
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
	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。
T4356	POL1-IN-1 Compound 3A	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	POL1-IN-1 (Compound 3A) 是一种RNA 聚合酶 1 POL1抑制剂，IC50值低于 0.5 uM。它能有效抑制A375恶性黑色素瘤细胞系中RNA 聚合酶I 的转录。
T70388	(S)-Enitociclib VIP152	CDK	Cell Cycle/Checkpoint
	(S)-Enitociclib (VIP152) 是一种选择性 CDK9 抑制剂，通过抑制 RNA 聚合酶 II 介导的转录来诱导 MYC+ 淋巴瘤的完全消退，抑制抗凋亡和促生存蛋白的转录。
T79404	A09-003	Apoptosis; BCL; CDK	Apoptosis; Cell Cycle/Checkpoint
	A09-003 是一种新型细胞周期蛋白依赖性激酶-9 CDK-9 抑制剂。A09-003 能够抑制多种白血病细胞系的增殖，抑制hi髓系细胞白血病序列-1蛋白增加。A09-003还能诱导细胞凋亡，降低 RNA 聚合酶 II 活性，降低 Mcl-1 表达。
T77520	AOH1996	Apoptosis; DNA/RNA Synthesis	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	AOH1996 是一种具有口服活性的复制体组分 PCNA (增殖细胞核抗原) 配体，靶向转录-复制冲突 (TRC)。AOH1996 可干扰 PCNA 与其结合蛋白的相互作用，导致 DNA 复制应激，诱导细胞凋亡 (apoptosis)。AOH1996 通过稳定 PCNA 和 RNA 聚合酶 II 的相互作用从而导致蛋白酶体依赖的 rpb1 降解和致命的 DNA 损伤。AOH1996 与 DNA 损伤剂具有协同作用，可抑制肿瘤细胞生长。
T40359	Thio-ITP 6-Thio-ITP,Thio-ITP,6-Mercaptopurine-riboside-5'-triphosphate,6-Thioinosine 5′-triphosphate
	Thio-ITP, also known as 6-Thioinosine 5'-triphosphate, is a competitive inhibitor of RNA polymerase activity. It exhibits a strong apparent affinity towards the polymerases, with Ki values of 40.9 μM for RNA polymerase I and 38.0 μM for RNA polymerase II.
T13540	alpha-Amanitin α-Amanitin,α-Amatoxin	Others	Others
	alpha-Amanitin is the principal toxin of poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.
T29453	5-Formylcytosine
	5-formylcytosine (5FC) is a rare base found in mammalian DNA. It participates in active DNA demethylation, changes DNA double helix structure, and reduces the transcription rate and substrate specificity of RNA polymerase II.
T18249	Mal-C6-α-Amanitin	Others	Others
	Mal-C6-α-Amanitin is a drug-linker conjugate for ADC with potent antitumor activity by using α-Amanitin (an RNA polymerase II inhibitor), linked via the ADC linker Mal-C6.
T13474	β-Amanitin	Others	Others
	β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom, and inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis.
T10436L	AZD4573 HCl (2057509-72-3 free base) AZD4573 hydrochloride,AZD4573,AZD4573 HCl,AZD-4573,AZD 4573
	AZD-4573 is a selective and short-acting inhibitor of the serine/threonine cyclin-dependent kinase 9, the catalytic subunit of the RNA polymerase II elongation factor positive transcription elongation factor b. It also has a potential antineoplastic activ
T36685	TAF 10 Peptide
	TAF10 is one of many protein factors or coactivators associated with RNA polymerase II activity. One vial of this peptide may be used as a methyltransferase acceptor peptide for more than 200 reactions at 15 μM.
T74659	Dideoxy-amanitin
	Dideoxy-amanitin (compound 2) 是一种α-Amanitin 衍生物，是一种强效和选择性的 RNA 聚合酶 II 变结构抑制剂，其 IC50值为 74.2 nM。
TP1683	[pSer2, pSer5, pSer7]-CTD
	[pSer2, pSer5, pSer7]-CTD is a substrate for CDK7(cyclin-dependent protein kinase), a phosphorylated polypeptide at ser2, ser5, and ser7 of RNA polymerase II carboxyl terminus (CTD).
TP1641	[pSer2, pSer5, pSer7]-CTD TFA
	[pSer2, pSer5, pSer7]-CTD (TFA) is a substrate for CDK7(cyclin-dependent protein kinase), a phosphorylated polypeptide at ser2, ser5, and ser7 of RNA polymerase II carboxyl terminus (CTD).
T83836	3'-O-Methylguanosine-5'-O-triphosphate sodium 3'-O-methyl GTP
	3'-O-Methylguanosine-5'-O-triphosphate（3'-O-methyl GTP）是GTP的甲基化衍生物，用作早期RNA聚合酶II延伸中间体制备中的链终止试剂。
T12135	Mycophenolic acid-d3 Mycophenolate-d3,Mycophenolate D3	Others; Antibacterial	Microbiology/Virology; Others
	Mycophenolic acid-d3 (Mycophenolate-d3) 是 Mycophenolic acid 的衍生物。Mycophenolic acid 是一种降低GTP 水平和损害RNA 聚合酶II (RNAP II)转录延伸的化合物，促进了近端位点的使用，能够逆转虫草素对选择性聚腺苷化的作用。
T69908	Pidnarulex HCl
	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...
T63841	BSJ-01-175
	BSJ-01-175 是选择性的、有效的 CDK12/13 共价抑制剂。BSJ-01-175 对癌细胞具有显著的选择性，对磷酸化RNA 聚合酶 II 表现出有效抑制作用，并能够显著下调 CDK12 靶向基因。
T69931	MFH290
	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 ...
T70988	Ibulocydine
	Ibulocydine is a potent CDK inhibitor. Ibulocydine has high activity against Cdk7/cyclin H/Mat1 and Cdk9/cyclin T. Ibulocydine inhibited the growth of HCC cells more effectively than other Cdk inhibitors, including olomoucine and roscovitine, whereas ibulocydine as well as the other Cdk inhibitors and BMK-Y101 minimally influenced the growth of normal hepatocyte cells. Ibulocydine induced apoptosis in HCC cells, most likely by inhibiting Cdk7 and Cdk9. In vitro treatment of HCC cells with ibuloc...
T36745	cDPCP
	cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when ad...
T63368	CDK7-IN-2
	CDK7-IN-2 是 CDK7 的有效抑制剂。其中 CDK7 利用 RNA 聚合酶 II (RNAPII) 的 Rbpl 亚基的磷酸化参与转录起始过程，其与细胞周期和转录活性的时间控制有关。CDK7 对癌症疾病，尤其是侵袭性和难以治疗的癌症具有研究潜力。
T62235	CDK-IN-9
	CDK-IN-9 (compound 24) 是一种 CDK 的有效抑制剂。CDK-IN-9 也是一种能够诱导 CDK12 和 DDB1 相互作用的分子胶，能够作用于 CDK2/E (IC50: 4 nM) 。CDK-IN-9 能够导致细胞周期蛋白 K (cyclin K) 的多泛素化及其随后的降解。CDK-IN-9 可以利用去磷酸化视网膜母细胞瘤蛋白和RNA 聚合酶 II，进而诱导细胞凋亡 (apoptosis)。
T73633	YKL-5-124 TFA
	YKL-5-124 TFA是一种高效、选择性不可逆的CDK7共价抑制剂，具有53.5 nM对CDK7的IC50值和9.7 nM对CDK7/Mat1/CycH的IC50值。此化合物对CDK7的选择性超过CDK9和CDK2 100倍以上，对CDK12和CDK13则无活性。YKL-5-124 TFA能显著诱导细胞周期停滞，抑制E2F驱动的基因表达，对RNA聚合酶II的磷酸化状态影响微乎其微。
T75303	Suramin
	Suramin为一种可逆的，竞争性PTPases抑制剂，有效抑制sirtuins：SirT1（IC50=297 nM），SirT2（IC50=1.15 μM），SirT5（IC50=22 μM）。同时，Suramin作为DNAtopoisomeraseII（IC50=5 μM）的竞争性逆转录酶抑制剂，以及SARS-CoV-2 RdRp有效抑制剂。此外，Suramin还能有效抑制IP5K，具有抗寄生虫、抗肿瘤及抗血管生成的作用。

化合物

Cat.No: T8972

Target: Others, DNA/RNA Synthesis, CDK, HSV

RNA polymerase II-IN-1

Cat.No: T74630

Target: DNA/RNA Synthesis

RNA polymerase II-IN-2

Cat.No: T74631

Cat.No: T4356

Synonym: Compound 3A

Target: DNA/RNA Synthesis

(S)-Enitociclib

Cat.No: T70388

Synonym: VIP152

Target: CDK

Cat.No: T79404

Target: Apoptosis, BCL, CDK

Cat.No: T77520

Target: Apoptosis, DNA/RNA Synthesis

Cat.No: T40359

Synonym: 6-Thio-ITP,Thio-ITP,6-Mercaptopurine-riboside-5'-triphosphate,6-Thioinosine 5′-triphosphate

Cat.No: T13540

Synonym: α-Amanitin,α-Amatoxin

Target: Others

5-Formylcytosine

Cat.No: T29453

Mal-C6-α-Amanitin

Cat.No: T18249

Target: Others

Cat.No: T13474

Target: Others

AZD4573 HCl (2057509-72-3 free base)

Cat.No: T10436L

Synonym: AZD4573 hydrochloride,AZD4573,AZD4573 HCl,AZD-4573,AZD 4573

Cat.No: T36685

Dideoxy-amanitin

Cat.No: T74659

[pSer2, pSer5, pSer7]-CTD

Cat.No: TP1683

[pSer2, pSer5, pSer7]-CTD TFA

Cat.No: TP1641

3'-O-Methylguanosine-5'-O-triphosphate sodium

Cat.No: T83836

Synonym: 3'-O-methyl GTP

Mycophenolic acid-d3

Cat.No: T12135

Synonym: Mycophenolate-d3,Mycophenolate D3

Target: Others, Antibacterial

Cat.No: T69908

Cat.No: T63841

Cat.No: T69931

Cat.No: T70988

Cat.No: T36745

Cat.No: T63368

Cat.No: T62235

Cat.No: T73633

Cat.No: T75303

Cat. No.	Product Name	Target	Signaling Pathways
T39649	ε-Amanitin
	ε-Amanitin is a cyclic peptide obtained from various mushroom species. It exhibits a strong affinity for RNA polymerase II and effectively inhibits its activity.
T39562	γ-Amanitin
	γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin.

天然产物

Cat.No: T39649

Cat.No: T39562

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