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BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNApolymeraseII phosphorylation, and downregulation of CDK12-targeted genes in cancer cells .
RNApolymeraseII-IN-1 (compound 19iv) is a amatoxin, inhibiting RNApolymeraseII (Pol II) with an IC50 value of 36.66 nM. RNApolymeraseII-IN-1 has higher cytotoxicity against cancer cells and less toxic in normal cells than α-Amanitin .
RNApolymeraseII-IN-2 (compound 20iii) is a potent RNApolymeraseII (Pol II) inhibitor with Ki value of 9.5 nM. RNApolymeraseII-IN-2 has cytotoxicity against cancer cells, and exhibits 2 and 5 fold toxicity than α-amanitin against CHO and HEK293 .
3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that inhibits DNA-dependent RNApolymerases I and II. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM .
γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNApolymeraseII and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin. γ-Amanitin competitively binds to monoclonal antibody (mAb), with an IC50 of 163.1 ng/mL .
CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNApolymeraseII. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12 .
Thio-ITP (6-Thioinosine 5′-triphosphate) is an RNApolymerase activity competitive inhibitor. Thio-ITP has a high apparent affinity for the polymerases (RNApolymerase I Ki: 40.9 μM; RNApolymeraseIIKi: 38.0 μM) .
Dideoxy-amanitin (compound 2), an α-Amanitin (HY-19610) derivative, is a potent and selective RNApolymeraseII allosteric inhibitor with an IC50 value of 74.2 nM .
Ethynylcytidine (ECyD), a nucleoside analog and a potent inhibitor of RNA synthesis, inhibits RNApolymerases I, II and II. Ethynylcytidine has robust antitumor activity in a wide range of models of cancer . Ethynylcytidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Mal-C6-α-Amanitin is a agent-linker conjugate for ADC with potent antitumor activity by using α-Amanitin (an RNApolymeraseII inhibitor), linked via the ADC linker Mal-C6.
3'-Deoxyuridine-5'-triphosphate trisodium (3'-dUTP trisodium) is a nucleotide analogue that inhibits DNA-dependent RNApolymerases I and II. 3'-Deoxyuridine-5'-triphosphate trisodium strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM .
[pSer2, pSer5, pSer7]-CTD (TFA), a substrate for CDK7 (cyclin dependent protein kinase), is a phosphorylated polypeptide at ser2, ser5 and ser7 sites of RNApolymeraseII carboxy-terminal domain (CTD) .
MFH290 is a potent and highly selective cyclin-dependent kinase 12/13 (CDK12/13) covalent inhibitor. MFH290 forms a covalent bond with Cys-1039 of CDK12 and exhibits excellent kinome selectivity and inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymeraseII (Pol II). MFH290 is used for cancer research .
Filibuvir is an orally active, selective non-nucleoside inhibitor of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNApolymerase (RdRp). Filibuvir binds noncovalently in the thumb II allosteric pocket of NS5B. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM for both isoforms, respectively . Filibuvir preferentially inhibits elongative RNA synthesis and potently decreases viral RNA accumulation .
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNApolymeraseII and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs) .
CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNApolymeraseII .
CDK7-IN-2 is a potent inhibitor of CDK7. CDK7 is implicated in both temporal control of the cell cycle and transcriptional activity. CDK7 is implicated in the transcriptional initiation process by phosphorylation of Rbpl subunit of RNAPolymeraseII (RNAPII). CDK7 has the potential for the research of cancer disease, in particular aggressive and hard- to-treat cancers (extracted from patent WO2019099298A1, compound 1) .
Fmoc-L-Asn(EDA-N3)-OH is a click chemistry reagent containing an azide group. This building block is reported in literature for the modification of Amanitin via Click Chemistry. Alpha-Amanitin is the deadliest member of the amatoxin peptide family produced by the death-cap mushroom A. phalloides. It is an orally available, rigid, bicyclic octapeptide and one of the most lethal known natural products (LD50 = 50-100 μg/kg) acting as highly selective allosteric inhibitor of the RNApolymeraseII .
Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin is a potent SARS-CoV-2 RNA-dependent RNApolymerase (RdRp) inhibitor .Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNApolymerase (RdRp) inhibitor . Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
MC-VC-PABC-C6-alpha-Amanitin is an antibody agent conjugate consisting of an anticancer toxin alpha-Amanitin (HY-19610) and a monoclonal antibody MC-VC-PABC-C6. Among them, alpha-Amanitin is a potent inhibitor of RNApolymeraseIIα. MC-VC-PABC-C6-alpha-Amanitin accurately targets HER2 receptors, specifically recognizes HER2-positive tumor cells. It is widely used in breast cancer and gastric cancer research .
YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNApolymeraseII phosphorylation status .
YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNApolymeraseII phosphorylation status .
Transcription is the essential first step in the conversion of the genetic information in the DNA into protein and the major point at which gene expression is controlled. Transcription of protein-coding genes is accomplished by the multi-subunit enzyme RNApolymeraseII and an ensemble of ancillary proteins, called transcription factors (TFs). Transcription factors play an important role in the long-term regulation of cell growth, differentiation and responses to environmental cues. Deregulated transcription factors contribute to the pathogenesis of a plethora of human diseases, ranging from diabetes, inflammatory disorders and cardiovascular disease to many cancers, and thus these proteins hold great therapeutic potential.
MCE offers a unique collection of 1288 compounds with validated transcription factor targets modulating properties. MCE transcription factor-targeted compound library is an effective tool for researching transcription factors as drug targets as well as modulation of TFs for different therapeutic applications.
[pSer2, pSer5, pSer7]-CTD, a substrate for CDK7 (cyclin dependent protein kinase), is a phosphorylated polypeptide at ser2, ser5 and ser7 sites of RNApolymeraseII carboxy-terminal domain (CTD) .
[pSer2, pSer5, pSer7]-CTD (TFA), a substrate for CDK7 (cyclin dependent protein kinase), is a phosphorylated polypeptide at ser2, ser5 and ser7 sites of RNApolymeraseII carboxy-terminal domain (CTD) .
3'-Deoxyuridine-5'-triphosphate trisodium (3'-dUTP trisodium) is a nucleotide analogue that inhibits DNA-dependent RNApolymerases I and II. 3'-Deoxyuridine-5'-triphosphate trisodium strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM .
3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that inhibits DNA-dependent RNApolymerases I and II. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM .
γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNApolymeraseII and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin. γ-Amanitin competitively binds to monoclonal antibody (mAb), with an IC50 of 163.1 ng/mL .
The TFIIF-related CTD phosphatase protein plays a key role in promoting RNA polymerase II activity by dephosphorylating "Ser-2" and "Ser-5" residues. This enhances the function of RNA polymerase II, allowing the protein to participate in the transcription process. TFIIF-associating CTD phosphatase Protein, Mouse (Myc, His) is the recombinant mouse-derived TFIIF-associating CTD phosphatase protein, expressed by E. coli , with N-His, C-Myc labeled tag. The total length of TFIIF-associating CTD phosphatase Protein, Mouse (Myc, His) is 164 a.a., with molecular weight of ~24.0 kDa.
TCEB3, also known as SIII, acts as a key transcription elongation factor that promotes RNA polymerase II progression beyond the blocking site. It interacts with SIII regulatory subunits B and C to form the elongin BC complex, which significantly enhances the transcriptional activity of subunit A. TCEB3 Protein, Human (Sf9) is the recombinant human-derived TCEB3 protein, expressed by Sf9 insect cells , with tag free. The total length of TCEB3 Protein, Human (Sf9) is 797 a.a., .
TCEB3, also known as SIII, acts as a key transcription elongation factor that promotes RNA polymerase II progression beyond the blocking site. It interacts with SIII regulatory subunits B and C to form the elongin BC complex, which significantly enhances the transcriptional activity of subunit A. TCEB3 Protein, Human (Sf9, His, Strep) is the recombinant human-derived TCEB3 protein, expressed by Sf9 insect cells , with N-Strep, N-8*His labeled tag. The total length of TCEB3 Protein, Human (Sf9, His, Strep) is 797 a.a., .
The PC4/SUB1 protein acts as a multifunctional coactivator that cooperates with TAF to promote functional interactions between upstream activators and the general transcription machinery. Its role extends to the potential stability of multiprotein transcription complexes. PC4/SUB1 Protein, Human (His) is the recombinant human-derived PC4/SUB1 protein, expressed by E. coli , with N-His labeled tag. The total length of PC4/SUB1 Protein, Human (His) is 127 a.a., with molecular weight of ~19 kDa.
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8-CCNC-MED12 Protein, Human (Sf9) is the recombinant human-derived CDK8-CCNC-MED12 protein, expressed by Sf9 insect cells , with tag free.
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8-CCNC-MED12 Protein, Human (Sf9, GST, FLAG, His) is the recombinant human-derived CDK8-CCNC-MED12 protein, expressed by Sf9 insect cells , with N-6*His, N-Flag, N-GST labeled tag.
CDK19 plays a key role in cellular homeostasis and developmental programming. CDK19 can interact with p53 to inhibit p53-mediated transcription of p21, and regulates the proliferation of hematopoietic stem cells and acute myeloid leukemia cells. Besides, CDK19 is the paralog of CDK8. CDK8 and CDK19 can cooperate with each other in stimulating NFκB-induced transcription and Dengue virus replication. CDK19-CCNC-MED12 Protein, Human (Sf9) is the recombinant human-derived CDK19-CCNC-MED12 protein, expressed by Sf9 insect cells , with tag free. ,
RNA Polymerase II Subunit B1 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 217 kDa, targeting to RNA Polymerase II Subunit B1. It can be used for WB,IHC-F,IHC-P,ICC/IF,IP assays with tag free, in the background of Human.
SKP1; EMC19; OCP2; SKP1A; TCEB1L; S-phase kinase-associated protein 1; Cyclin-A/CDK2-associated protein p19; Organ of Corti protein 2; OCP-2; Organ of Corti protein II; OCP-II; RNApolymeraseII elongation factor-like protein; SIII; Transcr
Ethynylcytidine (ECyD), a nucleoside analog and a potent inhibitor of RNA synthesis, inhibits RNApolymerases I, II and II. Ethynylcytidine has robust antitumor activity in a wide range of models of cancer . Ethynylcytidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Fmoc-L-Asn(EDA-N3)-OH is a click chemistry reagent containing an azide group. This building block is reported in literature for the modification of Amanitin via Click Chemistry. Alpha-Amanitin is the deadliest member of the amatoxin peptide family produced by the death-cap mushroom A. phalloides. It is an orally available, rigid, bicyclic octapeptide and one of the most lethal known natural products (LD50 = 50-100 μg/kg) acting as highly selective allosteric inhibitor of the RNApolymeraseII .
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