From 11:00 pm to 12:00 pm EST ( 8:00 pm to 9:00 pm PST ) on January 6th, the website will be under maintenance. We are sorry for the inconvenience. Please arrange your schedule properly.
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 .
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 .
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 .
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 .
CDKI-83 is a potent CDK9 and CDK1 inhibitor with Ki values of 21 nM and 72 nM for CDK9/T1 and CDK1/B, respectively. CDKI-83 demonstrates effective anti-proliferative activity in human tumour cell lines with a GI50<1 μM. CDKI-83 effectively induces apoptosis in A2780 human ovarian cancer cells. CDKI-83 reduces phosphorylation at Ser-2 of RNApolymeraseII (RNAPII) by inhibiting cellular CDK9 activity, and down-regulates Mcl-1 and Bcl-2. CDKI-83 has the potential for anti-cancer research .
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) .
CDK7-IN-30 (Compound 22) is a CDK7 inhibitor (IC50 = 7.21 nM) that effectively inhibits the phosphorylation of RNAPolymeraseII and CDK2. CDK7-IN-30 CDK7-IN-30 can induce cell apoptosis and has anti-cancer activity and can be used in cancer research .
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) .
Oncrasin-72 (NSC-743380) is an RNApolymeraseII inhibitor with activity in inhibiting growth and inducing cell death in human cancer cells. Oncrasin-72 exhibits antitumor activity through JNK activation and STAT3 inhibition. Analytical method development and validation for Oncrasin-72 is essential for quantifying its concentration in biological fluids for pharmacokinetic studies. This method was able to successfully quantify Oncrasin-72 in different dose groups when applied in rat plasma .
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 .
Suramin (sodium salt) (Standard) is the analytical standard of Suramin (sodium salt). This product is intended for research and analytical applications. 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 .
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 .
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 . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
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 1,403 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) .
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 .
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 .
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 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.
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 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-CCNK Protein, Human (sf9, GST) is the recombinant human-derived CDK8-CCNK, expressed by Sf9 insect cells , with N-GST labeled tag. ,
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 Protein, Human ( Unactive, sf9, GST) is the recombinant human-derived CDK8, expressed by Sf9 insect cells , with GST labeled tag. The total length of CDK8 Protein, Human ( Unactive, sf9, GST) is 464 a.a.,
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.
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 Protein, Human (Sf9) is the recombinant human-derived CDK8, expressed by Sf9 insect cells , with tag Free labeled tag. The total length of CDK8 Protein, Human (Sf9) is 464 a.a.,
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.
RNA Polymerase II Subunit B3 Antibody (YA2447) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2447), targeting RNA Polymerase II Subunit B3, with a predicted molecular weight of 31 kDa (observed band size: 31 kDa). RNA Polymerase II Subunit B3 Antibody (YA2447) can be used for WB, IHC-P experiment in human, mouse, rat background.
Transcription Initiation Factor IIB Antibody (YA1055) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1055), targeting Transcription Initiation Factor IIB, with a predicted molecular weight of 35 kDa (observed band size: 31 kDa). Transcription Initiation Factor IIB Antibody (YA1055) can be used for WB, IP experiment in human, mouse, rat background.
Transcription Initiation Factor IIB Antibody (YA1054) is a biotin-conjugated non-conjugated IgG2b antibody, targeting Transcription Initiation Factor IIB, with a predicted molecular weight of 35 kDa (observed band size: 35 kDa). Transcription Initiation Factor IIB Antibody (YA1054) can be used for WB experiment in human, mouse, monkey background.
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
WB, ICC/IF
Human, Mouse, Rat
SKP1 Antibody (YA1974) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1974), targeting SKP1, with a predicted molecular weight of 19 kDa (observed band size: 19 kDa). SKP1 Antibody (YA1974) can be used for WB, ICC/IF experiment in human, mouse, rat background.
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 . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
Inquiry Online
Your information is safe with us. * Required Fields.