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Isodiospyrin, a natural dimeric naphthoquinone, is a human DNAtopoisomeraseI(Topoisomerase) inhibitor. Isodiospyrin can prevent both DNA relaxation and kinase activities of human topoisomeraseI. Isodiospyrin shows anticancer, antibacterial and antifungal activities .
Camptothecin (CPT), a kind of alkaloid, is a DNAtopoisomeraseI (TopoI) inhibitor with an IC50 of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .
CL2A-SN-38 is a agent-linker conjugate composed of a potent a DNATopoisomeraseI inhibitor SN-38 and a linker CL2A to make antibody agent conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A-SN-38 uses hydrolyzable linker to deliver active agents within tumor cells and in the tumor microenvironment, resulting in bystander effects .
9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a novel camptothecin derivatives. 9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a DNAtopoisomeraseI (TopoI) inhibitor, can be used in anticancer research .
Irinotecan-d10 (hydrochloride) is the deuterium labeled Irinotecan. Irinotecan ((+)-Irinotecan) is a topoisomeraseI inhibitor, preventing religation of the DNA strand by binding to topoisomeraseI-DNA complex[1][2].
Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomeraseI inhibitor, preventing religation of the DNA strand by binding to topoisomeraseI-DNA complex[1].
TopoisomeraseI inhibitor 3 (Compound ZML-14) is a topoisomeraseI inhibitor and can interact with topoisomeraseI-DNA complex. TopoisomeraseI inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase .
Batracylin (NSC320846) is a potent DNATopoisomerasesI and DNATopoisomerases II inhibitor. Batracylin shows cytotoxicity and antiproliferative activity. Batracylin induces DNA breaks .
TopoisomeraseI inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. TopoisomeraseI inhibitor 5 can interfere with DNA and significantly inhibit the activity of TopoisomeraseI. TopoisomeraseI inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. TopoisomeraseI inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin .
TopoisomeraseI inhibitor 6 (Compound 3) is a potent inhibitor of TopoisomeraseI. TopoisomeraseI inhibitor 6 is able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line. TopoisomeraseI inhibitor 6 has the potential for the research of cancer diseases .
T-2513 is a selective topoisomeraseI inhibitor. T-2513 binds covalently to and stabilizes the topoisomeraseI-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death .
T-2513 hydrochloride is a selective topoisomeraseI inhibitor. T-2513 hydrochloride binds covalently to and stabilizes the topoisomeraseI-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death .
Rebeccamycin, an antitumor antibiotic, inhibits DNAtopoisomeraseI. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomeraseI and has negligible effect on protein kinase C and topoisomerase II .
TopoisomeraseI inhibitor 21 (Compound 3e) is an inhibitor for TopoisomeraseI through stabilization of enzyme-DNA complex. TopoisomeraseI inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM .
DACA inhibits two essential nuclear enzymes in vitro, DNAtopoisomeraseI and DNAtopoisomerase (topo) II. DACA stabilises topoI, topo II alpha, and topo II beta cleavable complexes in human leukaemia CCRF-CEM cells .
TopoisomeraseI/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). TopoisomeraseI/II inhibitor 2 has dual inhibition on DNAtopoisomeraseI/II, also can obviously reduce the growth of xenograft tumor in mice model. TopoisomeraseI/II inhibitor 2 has the potential value in researching liver cancer .
Becatecarin is a rebeccamycin analog with antitumor effects. Becatecarin intercalates into DNA and inhibites the catalytic activity of topoisomerasesI/II.
12-Ethyl-9-hydroxycamptothecin is a derivative of Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNAtopoisomeraseI (TopoI) inhibitor with an IC50 of 679 nM .
Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomeraseI poison and induces Top I mediated DNA cleavage . Coralyne chloride can be used for preparing coralyne derivatives as DNA binding fluorescent probes .
Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human DNAtopoisomeraseI and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomeraseI inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells .
Podocarpusflavone A is a DNAtopoisomeraseI inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor agents .
Doxorubicinone-d3 is the deuterium labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin[1]. Doxorubicin is a potent human DNAtopoisomeraseI and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
Dxd (Exatecan derivative for ADC) is a potent DNAtopoisomeraseI inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNAtopoisomeraseI and II inhibitor. Intoplicine strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA .
Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNAtopoisomeraseI inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
Belotecan (CKD-602 free base) is a DNAtopoisomeraseI inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer .
(S)-Benzyl 2-cyclopropyl-2-hydroxyacetate is an intermediate reactant in the synthesis of Camptothecin (HY-16560). Camptothecin is an inhibitor of the DNAtopoisomeraseTopoI, withIC50=679 nM .
Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNAtopoisomeraseI and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA .
SN-38 is an active metabolite of the TopoisomeraseI inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively .
MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is a agent-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNATopoisomeraseI inhibitor (IC50=2.2 μM) .
MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is a agent-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNATopoisomeraseI inhibitor (IC50=2.2 μM) .
SN38-COOH is used for the synthesis of antibody-drug conjugates (ADCs). SN-38 is an active metabolite of the TopoisomeraseI inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis .
Ac-Exatecan is acetylated Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNAtopoisomeraseI (IC50=2.2 μM) .
Doxorubicin (Hydroxydaunorubicin), a broad-spectrum anthracycline antibiotic with cytotoxic properties, is an anti-cancer chemotherapy agent. Doxorubicin has fluorescence properties. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy . Doxorubicin inhibits human DNAtopoisomeraseI with an IC50 of 0.8 μM .
Exatecan analog 36 is a analog of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNAtopoisomeraseI (IC50=2.2 μM) .
Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNAtopoisomeraseI and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy .
Groenlandicine is a protoberberine alkaloid isolated from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR) . Groenlandicine selectively induces topoisomeraseI-mediated DNA cleavage .
Dxd-d5 is a deuterium labeled Dxd. Dxd is a potent DNAtopoisomeraseI inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) [1].
Exatecan intermediate 8 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNAtopoisomeraseI (IC50=2.2 μM) .
Exatecan intermediate 9 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNAtopoisomeraseI (IC50=2.2 μM) .
Exatecan intermediate 11 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNAtopoisomeraseI (IC50=2.2 μM) .
Exatecan intermediate 10 is an intermediate in the synthesis of Exatecan (HY-13631).Exatecan (DX-8951) is a DNAtopoisomeraseI inhibitor with an IC50 of 2 .2 μM (0 .975 μg/mL) for use in cancer research .
Val-Cit-PAB-DEA-Dxd (compound 81) is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule Dxd (DNAtopoisomeraseI inhibitor). Val-Cit-PAB-DEA-Dxd can be used for ADC synthesis .
Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNAtopoisomerasesI and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent .
Propargyl-PEG4-GGFG-DXd is a drug-linker conjugate for ADC. Propargyl-PEG4-GGFG-DXd contains a ADC linker and a DNAtopoisomeraseI inhibitor DXd (HY-13631D) .
MC-SN38 is a agent-linker conjugate composed of a potent microtubule-disrupting agent SN38 and a non-cleavable MC linker to make antibody agent conjugate (ADC). SN-38, an active metabolite of the TopoisomeraseI inhibitor Irinotecan, inhibits DNA synthesis and causes frequent DNA single-strand breaks .
Mc-VC-PAB-SN38 consists a cleavable ADC linker (Mc-VC-PAB) and a DNAtopoisomeraseI inhibitor (SN38). Mc-VC-PAB-SN38 can be used in the synthesis of antibody-drug conjugates (ADCs) .
erythro-Austrobailignan-6 is an orally active anti-cancer agent. erythro-Austrobailignan-6 inhibits DNAtopoisomeraseI and II activity. erythro-Austrobailignan-6 induces cell apoptosis and increases phosphorylation of p38 and JNK .
Val-Cit-PAB-Exatecan (Val-Cit-PAB-DX8951) is a agent-linker conjugate for ADC. Val-Cit-PAB-Exatecan is composed of a DNAtopoisomeraseI DX-8951 (HY-13631) and a cathepsin cleavable ADC linker .
MC-Val-Cit-PAB-Exatecan (MC-Val-Cit-PAB-DX8951) is a agent-linker conjugate for ADC. MC-Val-Cit-PAB-Exatecan is composed of a DNAtopoisomeraseI DX-8951 (HY-13631) and a cathepsin cleavable ADC linker.
DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNAtopoisomeraseI. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-agent resistance (MDR) phenotype .
NH2-methylpropanamide-Exatecan TFA is a methylpropanamide-modified Exatecan (HY-13631), which is the common ADC Cytotoxin used in the synthesis of ADC. Exatecan is a DNAtopoisomeraseI inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research .
Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent TopoisomeraseI inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNAtopoisomeraseI with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein) .
MC-VA-PAB-Exatecan is a agent-linker conjugate for ADC. MC-VA-PAB-Exatecan contains the ADC linker (peptide MC-VA-PAB) and a DNAtopoisomeraseI inhibitor Exatecan (HY-13631). MC-VA-PAB-Exatecan synthesized ADC shows good antitumor activity .
Exatecan Intermediate 5 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNAtopoisomeraseI inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 5 can be used to synthesize Antibody-Drug Conjugates (ADCs).
Exatecan Intermediate 6 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNAtopoisomeraseI inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 6 can be used to synthesize Antibody-Drug Conjugates (ADCs).
Exatecan Intermediate 7 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNAtopoisomeraseI inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 7 can be used to synthesize Antibody-Drug Conjugates (ADCs).
Exatecan Intermediate 3 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNAtopoisomeraseI inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 3 can be used to synthesize Antibody-Drug Conjugates (ADCs).
Gly-Gly-Phe-Gly-NH-O-CO-Exatecan, as a drug-linker conjugate composed of linker Gly-Gly-Phe-Gly-NH-O-CO and Exatecan, can be used to prepare antibody conjugate drugs. Exatecan is a DNAtopoisomeraseI inhibitor that can be used in cancer research .
Cu(II)-Elesclomol is a Cu 2+ complex of Elesclomol (HY-12040). Cu(II)-Elesclomol induces cuproptosis. Cu(II)-Elesclomol also inducesapoptosis, causes a G1 cell cycle block and induces DNA double strand breaks in K562 cells. Cu(II)-Elesclomol also weakly inhibits DNAtopoisomeraseI. Cu(II)-Elesclomol has anticancer activity .
CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNAtopoisomeraseI with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein) .
Datopotamab (CDP7657) is an antibody targeting to TROP2. Datopotamab can be used to synthesize Datopotamab deruxtecan (HY-141598), TROP2-directed antibody-drug conjugate (ADC). Datopotamab deruxtecan consists of DNAtopoisomeraseI inhibitor Deruxtecan (HY-13631E) and Datopotamab .
XRD-0394 is a potent and specific dual inhibitor of ATM and DNA-PKcs with oral activity. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. In addition, XRD-0394 can potentiate the effects of PARP and topoisomeraseI inhibitors in vitro .
MC-GGFG-Exatecan (MC-GGFG-DX8951) is a agent-linker conjugate for ADC. MC-GGFG-Exatecan is a DX8951 (a DNAtopoisomeraseI inhibitor) derivative with protease cleavable MC-GGFG linker. MC-GGFG-Exatecan shows antitumor activity and can be used to prepare DX8951 antibody conjugate (ADC) .
MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan is a agent-linker conjugate for ADC, contains the ADC linker (MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic acid) and a DNAtopoisomeraseI inhibitor Exatecan (HY-13631). MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan synthesized ADC can be used in study of cancer .
Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNAtopoisomeraseI (TopoI) inhibitor with an IC50 of 679 nM[1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells[2][3].
(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNAtopoisomeraseI with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research .
SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the TopoisomeraseI inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively[1][2][3][4].
Gly-Cyclopropane-Exatecan involves in the synthesis of anti-B7-H4 ADC, containing Exatecan (HY-13631), a DNATopoisomeraseI inhibitor. Gly-Cyclopropane-Exatecan participated in the formation of the ADC hu2F7-Exatecan (compound 34), which showed antitumor activity in vivo and in vitro .
(1R,9R)-Exatecan mesylate((1R,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNAtopoisomeraseI with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research .
(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNAtopoisomeraseI inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment .
MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNAtopoisomeraseI inhibitor) agent linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.Albumin-coupled MAC glucosidol-linked SN-38 shows good stability in mouse plasma .
DBCO-PEG4-GGFG-Dxd is a agent-linker conjugate for ADC with potent antitumor activity by using Dxd (a DNAtopoisomeraseI inhibitor), linked via the cleavable ADC linker DBCO-PEG4-GGFG . DBCO-PEG4-GGFG-Dxd is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNAtopoisomeraseI inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNAtopoisomeraseI inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
Datopotamab (CDP7657) is an antibody targeting to TROP2. Datopotamab can be used to synthesize Datopotamab deruxtecan (HY-141598), TROP2-directed antibody-drug conjugate (ADC). Datopotamab deruxtecan consists of DNAtopoisomeraseI inhibitor Deruxtecan (HY-13631E) and Datopotamab .
Isodiospyrin, a natural dimeric naphthoquinone, is a human DNAtopoisomeraseI(Topoisomerase) inhibitor. Isodiospyrin can prevent both DNA relaxation and kinase activities of human topoisomeraseI. Isodiospyrin shows anticancer, antibacterial and antifungal activities .
Camptothecin (CPT), a kind of alkaloid, is a DNAtopoisomeraseI (TopoI) inhibitor with an IC50 of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .
12-Ethyl-9-hydroxycamptothecin is a derivative of Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNAtopoisomeraseI (TopoI) inhibitor with an IC50 of 679 nM .
Rebeccamycin, an antitumor antibiotic, inhibits DNAtopoisomeraseI. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomeraseI and has negligible effect on protein kinase C and topoisomerase II .
Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human DNAtopoisomeraseI and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomeraseI inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells .
SN-38 is an active metabolite of the TopoisomeraseI inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively .
Doxorubicin (Hydroxydaunorubicin), a broad-spectrum anthracycline antibiotic with cytotoxic properties, is an anti-cancer chemotherapy agent. Doxorubicin has fluorescence properties. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy . Doxorubicin inhibits human DNAtopoisomeraseI with an IC50 of 0.8 μM .
Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNAtopoisomeraseI and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy .
Groenlandicine is a protoberberine alkaloid isolated from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR) . Groenlandicine selectively induces topoisomeraseI-mediated DNA cleavage .
erythro-Austrobailignan-6 is an orally active anti-cancer agent. erythro-Austrobailignan-6 inhibits DNAtopoisomeraseI and II activity. erythro-Austrobailignan-6 induces cell apoptosis and increases phosphorylation of p38 and JNK .
(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNAtopoisomeraseI inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment .
The TOP1 protein is critical in cellular processes, mitigating DNA supercoiling and torsional tension during replication and transcription. It does this by transiently cutting and rejoining a DNA strand, introducing breaks through transesterification. TOP1 Protein, Human (765a.a, sf9, His) is the recombinant human-derived TOP1 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of TOP1 Protein, Human (765a.a, sf9, His) is 765 a.a., with molecular weight of ~93.1 kDa.
The TOP1 protein is critical in cellular processes, mitigating DNA supercoiling and torsional tension during replication and transcription. It does this by transiently cutting and rejoining a DNA strand, introducing breaks through transesterification. TOP1 Protein, Human (575a.a, sf9, His) is the recombinant human-derived TOP1 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of TOP1 Protein, Human (575a.a, sf9, His) is 575 a.a., with molecular weight of ~70.4 kDa.
Irinotecan-d10 (hydrochloride) is the deuterium labeled Irinotecan. Irinotecan ((+)-Irinotecan) is a topoisomeraseI inhibitor, preventing religation of the DNA strand by binding to topoisomeraseI-DNA complex[1][2].
Dxd-d5 is a deuterium labeled Dxd. Dxd is a potent DNAtopoisomeraseI inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) [1].
Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomeraseI inhibitor, preventing religation of the DNA strand by binding to topoisomeraseI-DNA complex[1].
Doxorubicinone-d3 is the deuterium labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin[1]. Doxorubicin is a potent human DNAtopoisomeraseI and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNAtopoisomeraseI (TopoI) inhibitor with an IC50 of 679 nM[1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells[2][3].
SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the TopoisomeraseI inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively[1][2][3][4].
DBCO-PEG4-GGFG-Dxd is a agent-linker conjugate for ADC with potent antitumor activity by using Dxd (a DNAtopoisomeraseI inhibitor), linked via the cleavable ADC linker DBCO-PEG4-GGFG . DBCO-PEG4-GGFG-Dxd is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
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