Search Result
Results for "
topoisomerase-I
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
10
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-156969
-
|
Topoisomerase
Btk
|
Cancer
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Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 11 can bind to BTK .
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-
-
- HY-148058
-
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Topoisomerase
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Cancer
|
Topoisomerase I inhibitor 8 is a potent topoisomerase I inhibitor. Topoisomerase I inhibitor 8 is a hexacyclic analogue of camptothecin, and displays cytotoxic effect against tumor cells .
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-
-
- HY-143266
-
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Topoisomerase
Apoptosis
|
Cancer
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Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase .
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-
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- HY-144774
-
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Topoisomerase
DNA/RNA Synthesis
Apoptosis
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Cancer
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Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin .
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-
-
- HY-161082
-
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Topoisomerase
|
Cancer
|
Topoisomerase I inhibitor 12 (compound 12), a Camptothecin (HY-16560)-based derivative, is a potent Topoisomerase I inhibitor. Topoisomerase I inhibitor 12 shows anticancer activity .
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-
-
- HY-162341
-
|
Topoisomerase
|
Cancer
|
Topoisomerase I inhibitor 15 (compound 4b) is an inhibitor of topoisomerase I with anticancer activity. Topoisomerase I inhibitor 15 inhibits A549 cells with an IC50 of 7.34 μM .
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-
-
- HY-146437
-
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Topoisomerase
|
Cancer
|
Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 6 is able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line. Topoisomerase I inhibitor 6 has the potential for the research of cancer diseases .
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-
-
- HY-143265
-
|
Topoisomerase
Apoptosis
Caspase
|
Cancer
|
Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect .
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-
-
- HY-146497
-
|
Topoisomerase
|
Cancer
|
Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor agent candidates among the heteroarene-fused anthraquinones .
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-
-
- HY-143301
-
|
Topoisomerase
|
Cancer
|
Topoisomerase I inhibitor 4 (compound 7a) is a topoisomerase I inhibitor. Topoisomerase I inhibitor 4 inhibits HepG2, A549, MCF-7 and HeLa cancer cells proliferation with IC50s of 1.20, 2.09, 1.56 and 1.92 μM, respectively. Topoisomerase I inhibitor 4 can be used for the research of cancer .
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-
-
- HY-161385
-
|
Topoisomerase
|
Cancer
|
Topoisomerase I inhibitor 21 (Compound 3e) is an inhibitor for Topoisomerase I through stabilization of enzyme-DNA complex. Topoisomerase I inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM .
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-
-
- HY-149002
-
|
Topoisomerase
Apoptosis
|
Cancer
|
Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research .
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-
-
- HY-162091
-
|
Topoisomerase
|
Cancer
|
Topoisomerase I inhibitor 13 (Compound G11) is a Topo I inhibitor that inhibits cancer cell proliferation. Topoisomerase I inhibitor 13 significantly inhibits tumor growth in vivo .
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-
-
- HY-146504
-
|
Topoisomerase
PI3K
Apoptosis
Reactive Oxygen Species
|
Cancer
|
Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Topoisomerase I/II inhibitor 3 can be used for liver cancer research .
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-
-
- HY-156464
-
|
Topoisomerase
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Infection
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Topoisomerase I inhibitor 10 (compound 13) is a leishmanial topoisomerase IB inhibitor. Topoisomerase I inhibitor 10 has antileishmanial activity against L. donovani promastigotes, with the IC50 of 27.91 μM .
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-
-
- HY-162342
-
|
Topoisomerase
|
Cancer
|
Topoisomerase I inhibitor 14 (Compound 4h) is an inhibitor for Topoisomerase I. Topoisomerase I inhibitor 14 inhibits proliferation of A549 and C6 with IC50s of 4.56 μM and 13.17 μM, without significant toxicity in healthy cells NIH3T3 (IC50 is 74.44 μM), which exhibits anticancer potency .
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-
-
- HY-143402
-
|
Topoisomerase
|
Cancer
|
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
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-
-
- HY-156462
-
|
Topoisomerase
|
Infection
|
Topoisomerase I inhibitor 9 (compound 3d) is a leishmanial topoisomerase IB inhibitor. Topoisomerase I inhibitor 9 has antileishmanial activity against L. donovani promastigotes, with the IC50 of 34.81μM .
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-
-
- HY-16562
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(+)-Irinotecan; CPT-11; VAL-413(free base)
|
Topoisomerase
Autophagy
|
Cancer
|
Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
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-
-
- HY-16562S1
-
|
Isotope-Labeled Compounds
Topoisomerase
Autophagy
|
Cancer
|
Irinotecan-d10 (hydrochloride) is the deuterium labeled Irinotecan. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex[1][2].
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-
-
- HY-16562S
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(+)-Irinotecan-d10; CPT-11-d10; VAL-413-d10
|
Topoisomerase
Autophagy
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Cancer
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Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex[1].
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-
-
- HY-19825
-
|
Topoisomerase
ADC Cytotoxin
Antibiotic
|
Cancer
|
Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II .
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- HY-125930
-
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Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
T-2513 is a selective topoisomerase I inhibitor. T-2513 binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death .
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-
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- HY-125930A
-
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Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
T-2513 hydrochloride is a selective topoisomerase I inhibitor. T-2513 hydrochloride binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death .
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-
- HY-14821
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ST-1968
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Topoisomerase
|
Cancer
|
Namitecan is a potent topoisomerase I inhibitor, with antitumor property.
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-
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- HY-N3488
-
|
Topoisomerase
Bacterial
Fungal
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Infection
Cancer
|
Isodiospyrin, a natural dimeric naphthoquinone, is a human DNA topoisomerase I (Topoisomerase) inhibitor. Isodiospyrin can prevent both DNA relaxation and kinase activities of human topoisomerase I. Isodiospyrin shows anticancer, antibacterial and antifungal activities .
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-
- HY-13768A
-
SKF 104864A hydrochloride; NSC 609669 hydrochloride
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.
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-
-
- HY-14812
-
Cositecan; BNP 1350
|
Topoisomerase
|
Cancer
|
Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity.
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-
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- HY-N10115
-
-
-
- HY-16568
-
(+)-Irinotecan hydrochloride trihydrate; CPT-11 hydrochloride trihydrate
|
Topoisomerase
Autophagy
|
Cancer
|
Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate) is a topoisomerase I inhibitor with antitumor activity .
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-
- HY-13566A
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CKD-602
|
Topoisomerase
|
Cancer
|
Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative.
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-
-
- HY-13622A
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BN 80927 free base
|
Topoisomerase
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Cancer
|
Elomotecan (BN 80927 free base) is a potent inhibitor of topoisomerases I and II. Elomotecan is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II .
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-
-
- HY-16228
-
|
Topoisomerase
|
Cancer
|
Genz-644282 is a non-camptothecin topoisomerase I inhibitor, used for cancer research.
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-
-
- HY-18350
-
LMP776
|
Topoisomerase
|
Cancer
|
Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities .
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-
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- HY-13622
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BN 80927
|
Topoisomerase
|
Cancer
|
Elomotecan hydrochloride (BN 80927) is a potent inhibitor of topoisomerases I and II. Elomotecan hydrochloride (BN 80927) is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan hydrochloride (BN 80927) reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II .
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-
-
- HY-13758A
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BMS-247615 dihydrochloride
|
Topoisomerase
|
Cancer
|
TAS-103 dihydrochloride is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
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-
-
- HY-13758
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BMS-247615
|
Topoisomerase
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Cancer
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TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
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-
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- HY-13618
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J 107088; PF 804950
|
Topoisomerase
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Cancer
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Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM.
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-
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- HY-16562A
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(+)-Irinotecan hydrochloride; CPT-11 hydrochloride; VAL-413
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Topoisomerase
Autophagy
|
Cancer
|
Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer .
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- HY-N2331
-
|
|
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Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively .
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-
-
- HY-100309
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9-Amino-20(S)-camptothecin; 9-Amino-CPT
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Topoisomerase
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Cancer
|
9-Aminocamptothecin (9-Amino-CPT) is a topoisomerase I inhibitor with potent anticancer activity .
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-
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- HY-N0275
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(±)-10-HCPT
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Topoisomerase
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Cancer
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(±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.
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-
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- HY-13565
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NSC 655649; BMS 181176; BMY 27557
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Topoisomerase
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Cancer
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Becatecarin is a rebeccamycin analog with antitumor effects. Becatecarin intercalates into DNA and inhibites the catalytic activity of topoisomerases I/II.
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- HY-N5038
-
|
Topoisomerase
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Cancer
|
Mauritianin is a kaempferol glycoside isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor .
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-
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- HY-B0063
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ST1481
|
Topoisomerase
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Cancer
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Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity .
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-
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- HY-U00248A
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MJ-III65 hydrochloride; NSC706744 hydrochloride
|
Topoisomerase
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Cancer
|
LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity .
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-
-
- HY-U00248
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MJ-III65; NSC706744
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Topoisomerase
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Cancer
|
LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity .
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-
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- HY-120185
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UCT-1003
|
Topoisomerase
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Infection
Cancer
|
Saintopin is an antitumor antibiotic. Saintopin is also an inhibitor of DNA topoisomerases I and II. Saintopin induces DNA cleavage .
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-
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- HY-126142
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-
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- HY-N10367
-
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Topoisomerase
|
Cancer
|
Corydamine, 3-arylisoquinoline alkaloid, is a potent DNA topoisomerase I/II inhibitor. Corydamine has anti-cancer activity .
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- HY-13670
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GI147211; OSI-211
|
Topoisomerase
|
Cancer
|
Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects .
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- HY-19637
-
|
Topoisomerase
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Cancer
|
SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
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- HY-13631AS
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DX8951f-d5; Exatecan-d5 mesylate; Deuterated labeled Exatecan mesylate
|
ADC Cytotoxin
Topoisomerase
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Cancer
|
Exatecan-d5 (mesylate) is deuterium labeled Exatecan mesylate. Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL[1].
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- HY-13631
-
DX-8951
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
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- HY-107133
-
|
Topoisomerase
Cytochrome P450
|
Cancer
|
Simmitecan hydrochloride, a 9-substituted lipophilic Camptothecin (HY-16560) derivative, is a potent topoisomerase I inhibitor. Simmitecan hydrochloride is an anticancer agent .
|
-
- HY-13631A
-
DX8951f
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
Exatecan mesylate (DX8951f) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research.
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-
- HY-13566AS
-
|
Topoisomerase
|
Cancer
|
Belotecan-d7 (hydrochloride) is the deuterium labeled Belotecan hydrochloride. Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative[1][2].
|
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- HY-126373
-
SN-38G
|
Drug Metabolite
|
Cancer
|
SN-38 glucuronide is an inactive metabolite of the cancer agent Irinotecan. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
|
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- HY-119892
-
NSC 320846; BAY-H 2049
|
Topoisomerase
|
Cancer
|
Batracylin (NSC320846) is a potent DNA Topoisomerases I and DNA Topoisomerases II inhibitor. Batracylin shows cytotoxicity and antiproliferative activity. Batracylin induces DNA breaks .
|
-
- HY-N6621
-
|
Topoisomerase
|
Cancer
|
Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities .
|
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- HY-N2063
-
|
Topoisomerase
|
Others
|
12-Ethyl-9-hydroxycamptothecin is a derivative of Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM .
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- HY-N2198
-
|
|
|
Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor agents .
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-
- HY-116933
-
|
Topoisomerase
Bacterial
|
Infection
Inflammation/Immunology
|
Murrayanol is a natural carbazole alkaloid with a variety of biological activities. Murrayanol shows anti-inflammatory, topoisomerase I and topoisomerase II (Topoisomerase) inhibition activities. Murrayanol also as a mosquitocidal and antimicrobial .
|
-
- HY-13631P
-
DX-8951 mesylate dihydrate
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
Exatecan (DX-8951) mesylate dihydrate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research .
|
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- HY-13555
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ARQ-501; NSC-26326
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.
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- HY-123143
-
MLN576
|
Topoisomerase
|
Cancer
|
XR11576 (MLN576) is an orally active inhibitor of topoisomerase I and II. XR11576 shows cytotoxicity against human and murine tumor cell lines (IC50: 6-47 nM) .
|
-
- HY-145078
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
PNU-EDA-Gly5 is an oligo-glycine linker-payload for ADC synthesis, composed of a DNA topoisomerase I inhibitor PNU-159682 and a linker EDA-Gly5 .
|
-
- HY-10529
-
-
- HY-13631D
-
Exatecan derivative for ADC
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
|
-
- HY-145513
-
|
Topoisomerase
|
Cancer
|
CL2-MMT-SN38 is a SN-38 derivative. SN-38, an anticancer agent, is an active metabolite of the Topoisomerase I inhibitor Irinotecan (CPT-11) .
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- HY-156402
-
|
Topoisomerase
|
Cancer
|
AuM1Gly is a topoisomerase I inhibitor. AuM1Gly affects the growth of MDA-MB-231 breast cancer cells, with IC50?values in the low nanomolar range .
|
-
- HY-13631AG
-
DX8951f
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
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-
- HY-13611
-
BN 80915
|
Topoisomerase
|
Cancer
|
Diflomotecan (BN 80915) is a potent and orally active inhibitor of topoisomerase I. Diflomotecan (BN 80915) causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds .
|
-
- HY-13768C
-
SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrate
|
Topoisomerase
Apoptosis
Autophagy
|
Cancer
|
Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity .
|
-
- HY-13566
-
CKD-602 free base
|
Topoisomerase
Apoptosis
|
Cancer
|
Belotecan (CKD-602 free base) is a DNA topoisomerase I 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 .
|
-
- HY-13704
-
7-Ethyl-10-hydroxycamptothecin
|
Topoisomerase
ADC Cytotoxin
Autophagy
|
Cancer
|
SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively .
|
-
- HY-148668
-
-
- HY-148668A
-
-
- HY-153013
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
SN38-COOH is used for the synthesis of antibody-drug conjugates (ADCs). SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis .
|
-
- HY-79490
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
Ac-Exatecan is acetylated Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM) .
|
-
- HY-100620
-
APC
|
Topoisomerase
Cholinesterase (ChE)
|
Cancer
|
RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE .
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-
- HY-13744
-
RFS 2000; 9-Nitrocamptothecin
|
Topoisomerase
|
Cancer
|
Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells .
|
-
- HY-121309
-
Adriamycin aglycone; Adriamycinone
|
Endogenous Metabolite
|
Cancer
|
Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
|
-
- HY-114983
-
(S)-9-Allyl-10-Hydroxycamptothecin
|
Topoisomerase
|
Cancer
|
Chimmitecan ((S)-9-Allyl-10-Hydroxycamptothecin), a novel 9-small-alkyl-substituted lipophilic Camptothecin (HY-16560), is a potent inhibitor of topoisomerase I. Chimmitecan exhibits anticancer activity .
|
-
- HY-48878
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
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 DNA topoisomerase I (IC50=2.2 μM) .
|
-
- HY-N6714
-
|
Topoisomerase
|
Infection
Cancer
|
Alternariol is a mycotoxin produced by Alternaria species. AOH inhibits the catalytic activity of topoisomerase I and topoisomerase II enzymes . Alternariol exhibits a variety of therapeutic and biological properties such as phytotoxicity, cytotoxicity, anti-HIV, anti-cancer, and anti-microbial properties .
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-
- HY-N6865
-
|
Topoisomerase
|
Metabolic Disease
Cancer
|
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 topoisomerase I-mediated DNA cleavage .
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-
- HY-118581
-
|
Topoisomerase
|
Cancer
|
Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage . Coralyne chloride can be used for preparing coralyne derivatives as DNA binding fluorescent probes .
|
-
- HY-13631DS
-
Exatecan-d5 derivative for ADC
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
Dxd-d5 is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) [1].
|
-
- HY-119458
-
|
Topoisomerase
TMV
Fungal
|
Infection
|
Luotonin A is an antiviral and antiphytopathogenic fungus agent. Luotonin A has good antiviral activity against tobacco mosaic virus (TMV). Luotonin A also has certain inhibitory activity on topoisomerase I and topoisomerase II. Luotonin A shows antitumor activity .
|
-
- HY-400316
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
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 DNA topoisomerase I (IC50=2.2 μM) .
|
-
- HY-43565
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
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 DNA topoisomerase I (IC50=2.2 μM) .
|
-
- HY-49861
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
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 DNA topoisomerase I (IC50=2.2 μM) .
|
-
- HY-43565B
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
Exatecan intermediate 10 is an intermediate in the synthesis of Exatecan (HY-13631).Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 of 2 .2 μM (0 .975 μg/mL) for use in cancer research .
|
-
- HY-158137
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
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 (DNA topoisomerase I inhibitor). Val-Cit-PAB-DEA-Dxd can be used for ADC synthesis .
|
-
- HY-13768
-
SKF 104864A; NSC 609669
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity .
|
-
- HY-135845
-
CH0793011
|
Topoisomerase
|
Cancer
|
TP3011 (CH0793011) is an active metabolite of CH-0793076 and is a potent topoisomerase I inhibitor equipotent as SN38 . TP3011 is against cancer cell lines growth with IC50s at the range sub-nanomolar in vitro .
|
-
- HY-156755
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
Propargyl-PEG4-GGFG-DXd is a drug-linker conjugate for ADC. Propargyl-PEG4-GGFG-DXd contains a ADC linker and a DNA topoisomerase I inhibitor DXd (HY-13631D) .
|
-
- HY-100777
-
|
|
|
DACA inhibits two essential nuclear enzymes in vitro, DNA topoisomerase I and DNA topoisomerase (topo) II. DACA stabilises topo I, topo II alpha, and topo II beta cleavable complexes in human leukaemia CCRF-CEM cells .
|
-
- HY-131057
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
Mc-VC-PAB-SN38 consists a cleavable ADC linker (Mc-VC-PAB) and a DNA topoisomerase I inhibitor (SN38). Mc-VC-PAB-SN38 can be used in the synthesis of antibody-drug conjugates (ADCs) .
|
-
- HY-N11536
-
|
Topoisomerase
Apoptosis
|
Cancer
|
erythro-Austrobailignan-6 is an orally active anti-cancer agent. erythro-Austrobailignan-6 inhibits DNA topoisomerase I and II activity. erythro-Austrobailignan-6 induces cell apoptosis and increases phosphorylation of p38 and JNK .
|
-
- HY-153031
-
Val-Cit-PAB-DX8951
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
Val-Cit-PAB-Exatecan (Val-Cit-PAB-DX8951) is a agent-linker conjugate for ADC. Val-Cit-PAB-Exatecan is composed of a DNA topoisomerase I DX-8951 (HY-13631) and a cathepsin cleavable ADC linker .
|
-
- HY-A0210
-
-
- HY-N2306
-
Aclarubicin
|
|
|
Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis .
|
-
- HY-N2306A
-
Aclarubicin hydrochloride
|
Topoisomerase
DNA/RNA Synthesis
Proteasome
Antibiotic
|
Cancer
|
Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis .
|
-
- HY-145929
-
MC-Val-Cit-PAB-DX8951
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
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 DNA topoisomerase I DX-8951 (HY-13631) and a cathepsin cleavable ADC linker.
|
-
- HY-156403
-
|
Topoisomerase
|
Cancer
|
AuM1Phe, an N-Heterocyclic carbene (NHC) metal complexe, blocks the human topoisomerase I activity and actin polymerization reaction. AuM1Phe affects the growth of MDA-MB-231 breast cancer cells, with an IC50 value of 1.2 μM .
|
-
- HY-125331
-
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-agent resistance (MDR) phenotype .
|
-
- HY-146094
-
|
Topoisomerase
|
Cancer
|
Antitumor agent-63 (Compound 40), a 20 (S)-O-linked camptothecin (CPT) glycoconjugate, is an antitumor agent without toxicity towards normal cells. Antitumor agent-63 shows high stability and very weak direct topoisomerase I (Topo I) inhibition .
|
-
- HY-148819
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (compound I) is a topoisomerase I inhibitor, which can be delivered to cells through conjugated antibody targeting, and has good ADC activity in vivo and in vitro .
|
-
- HY-148820
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (Formula V) is a agent-linker conjugate that composed of a potent topoisomerase I inhibitor and a linker to make antibody agent conjugate (ADC) .
|
-
- HY-148819A
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (compound I) hydrochloride is a topoisomerase I inhibitor, which can be delivered to cells through conjugated antibody targeting, and has good ADC activity in vivo and in vitro .
|
-
- HY-155034
-
|
Topoisomerase
GLUT
|
Cancer
|
Antitumor agent-102 (compound 10) is a conjugate of Topoisomerase I inhibitor SN38 and glucose transporter inhibitor, targeting to colorectal cancer. Antitumor agent-102 induces higher concentrations of free SN38 in tumor tissues than Irinotecan (HY-16562) .
|
-
- HY-147095
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
Val-Ala-PABC-Exatecan is a Drug-Linker Conjugates for ADC,consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (topoisomerase I inhibitor,HY-13631). Val-Ala-PABC-Exatecan can be used for ADC molecues synthesis,such as Mal-PEGn-amide-va-Exatecan .
|
-
- HY-139909
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
CL2E-SN-38, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor .
|
-
- HY-156686
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
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 DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research .
|
-
- HY-147095A
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
Val-Ala-PABC-Exatecan trifluoroacetate is a Drug-Linker Conjugates for ADC, consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (topoisomerase I inhibitor, HY-13631). Val-Ala-PABC-Exatecan trifluoroacetate can be used for ADC molecues synthesis, such as Mal-PEGn-amide-va-Exatecan .
|
-
- HY-18351
-
LMP-400; NSC-724998
|
Topoisomerase
|
Infection
Cancer
|
Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I 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 .
|
-
- HY-107096
-
TP3076
|
Topoisomerase
|
Cancer
|
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein) .
|
-
- HY-121309S
-
Adriamycin aglycone-d3; Adriamycinone-d3
|
Endogenous Metabolite
|
Cancer
|
Doxorubicinone-d3 is the deuterium labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin[1]. Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
|
-
- HY-139909A
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
CL2E-SN-38 TFA, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor .
|
-
- HY-147270
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
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 DNA topoisomerase I inhibitor Exatecan (HY-13631). MC-VA-PAB-Exatecan synthesized ADC shows good antitumor activity .
|
-
- HY-N10495
-
|
Antibiotic
Bacterial
Topoisomerase
|
Infection
|
Seconeolitsine, an antibiotic, and is an inhibitor of targeting topoisomerase I (TopA). Seconeolitsine also is a new antimicrobial agent that can inhibit S. pneumoniae growth. Seconeolitsine can inhibit TopA relaxation activity with an IC50 value of 17 μM. Seconeolitsine can be used for the research of S. pneumoniae infections resistant to other antibiotics .
|
-
- HY-43564
-
|
ADC Cytotoxin
Topoisomerase
|
|
Exatecan Intermediate 5 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I 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).
|
-
- HY-44369
-
|
ADC Cytotoxin
Topoisomerase
|
|
Exatecan Intermediate 6 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I 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).
|
-
- HY-45157
-
|
ADC Cytotoxin
Topoisomerase
|
|
Exatecan Intermediate 7 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I 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).
|
-
- HY-46081
-
|
ADC Cytotoxin
Topoisomerase
|
|
Exatecan Intermediate 3 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I 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).
|
-
- HY-156723
-
|
Topoisomerase
|
Cancer
|
9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a novel camptothecin derivatives. 9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a DNA topoisomerase I (Topo I) inhibitor, can be used in anticancer research .
|
-
- HY-13631F
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
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 DNA topoisomerase I inhibitor that can be used in cancer research .
|
-
- HY-126373S1
-
SN-38G-13C6
|
Isotope-Labeled Compounds
|
Others
|
SN-38 glucuronide- 13C6 is the 13C labeled SN-38 glucuronide (HY-126373) . SN-38 glucuronide is an inactive metabolite of the cancer agent Irinotecan. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
|
-
- HY-101647
-
RP 60475
|
Topoisomerase
|
Cancer
|
Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA .
|
-
- HY-B1099
-
|
DNA/RNA Synthesis
Topoisomerase
Parasite
|
Infection
|
Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I 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 .
|
-
- HY-107096B
-
TP3076 TFA
|
Topoisomerase
|
Cancer
|
CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein) .
|
-
- HY-P99843
-
|
TROP2
ADC Antibody
|
Cancer
|
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 DNA topoisomerase I inhibitor Deruxtecan (HY-13631E) and Datopotamab .
|
-
- HY-162472
-
|
ATM/ATR
DNA-PK
|
Cancer
|
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 topoisomerase I inhibitors in vitro .
|
-
- HY-136170
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
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 Topoisomerase I inhibitor Irinotecan, inhibits DNA synthesis and causes frequent DNA single-strand breaks .
|
-
- HY-114233
-
MC-GGFG-DX8951
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
MC-GGFG-Exatecan (MC-GGFG-DX8951) is a agent-linker conjugate for ADC. MC-GGFG-Exatecan is a DX8951 (a DNA topoisomerase I inhibitor) derivative with protease cleavable MC-GGFG linker. MC-GGFG-Exatecan shows antitumor activity and can be used to prepare DX8951 antibody conjugate (ADC) .
|
-
- HY-101647A
-
RP 60475 dimesylate
|
Topoisomerase
|
Cancer
|
Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA .
|
-
- HY-147307
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
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 DNA topoisomerase I inhibitor Exatecan (HY-13631). MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan synthesized ADC can be used in study of cancer .
|
-
- HY-P99813
-
HER3-DXd
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
Patritumab deruxtecan (HER3-DXd) is an antibody-drug conjugate (ADC) consisting of a fully human anti-HER3 IgG1 monoclonal antibody Patritumab (HY-P99275) attached to a topoisomerase I inhibitor payload via a tetrapeptide-based cleavable linker. Patritumab deruxtecan shows anticancer activity .
|
-
- HY-13631I
-
(1S,9R)-DX8951f
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research .
|
-
- HY-15142
-
Hydroxydaunorubicin hydrochloride
|
Topoisomerase
ADC Cytotoxin
AMPK
Autophagy
Apoptosis
HIV
HBV
Mitophagy
Antibiotic
Bacterial
|
Infection
Cancer
|
Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I 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 .
|
-
- HY-13704S
-
NK012-d3
|
Topoisomerase
ADC Cytotoxin
Autophagy
|
Cancer
|
SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively[1][2][3][4].
|
-
- HY-148696A
-
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
Gly-Cyclopropane-Exatecan involves in the synthesis of anti-B7-H4 ADC, containing Exatecan (HY-13631), a DNA Topoisomerase I inhibitor. Gly-Cyclopropane-Exatecan participated in the formation of the ADC hu2F7-Exatecan (compound 34), which showed antitumor activity in vivo and in vitro .
|
-
- HY-13631J
-
(1R,9R)-DX8951f
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
(1R,9R)-Exatecan mesylate((1R,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research .
|
-
- HY-16560
-
Campathecin; (S)-(+)-Camptothecin; CPT
|
Topoisomerase
ADC Cytotoxin
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Infection
Cancer
|
Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) 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 .
|
-
- HY-N0095
-
10-HCPT; 10-Hydroxycamptothecin
|
Topoisomerase
Apoptosis
|
Cancer
|
(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I 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 .
|
-
- HY-156376
-
|
Cuproptosis
Apoptosis
Topoisomerase
|
Cancer
|
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 DNA topoisomerase I. Cu(II)-Elesclomol has anticancer activity .
|
-
- HY-128942
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 agent linker. MAC glucuronide α-hydroxy lactone-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 99 and 105 ng/mL, respectively .
|
-
- HY-13768S1
-
|
Isotope-Labeled Compounds
Topoisomerase
Autophagy
|
Cancer
|
Topotecan-d6 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95 μM of GSCs-U87[1][2].
|
-
- HY-138298A
-
DS-8201; DS-8201a
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, a topoisomerase I inhibitor (a toxin component of Dxd). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .
|
-
- HY-16560S
-
Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5
|
Topoisomerase
ADC Cytotoxin
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Infection
Cancer
|
Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) 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].
|
-
- HY-128943
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I 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 .
|
-
- HY-134723
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
DBCO-PEG4-GGFG-Dxd is a agent-linker conjugate for ADC with potent antitumor activity by using Dxd (a DNA topoisomerase I 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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- HY-138298
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DS-8201 (solution); DS-8201a (solution)
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Antibody-Drug Conjugates (ADCs)
EGFR
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Cancer
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Trastuzumab deruxtecan (T-DXd; DS-8201a) (solution) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, a topoisomerase I inhibitor (a toxin component of Dxd). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .
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- HY-15142A
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Hydroxydaunorubicin
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ADC Cytotoxin
Antibiotic
Bacterial
Topoisomerase
AMPK
HIV
Autophagy
Mitophagy
Apoptosis
HBV
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Infection
Cancer
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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 DNA topoisomerase I with an IC50 of 0.8 μM .
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- HY-128946
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Drug-Linker Conjugates for ADC
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Inflammation/Immunology
Cancer
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CL2A-SN-38 is a agent-linker conjugate composed of a potent a DNA Topoisomerase I 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 .
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- HY-155073
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM). Tubulin inhibitor 35 inhibits migration and invasion of MGC-803 and RKO cell lines,and induces apoptosis via arresting cell cycle at G2/M phase. Tubulin inhibitor 35 exhibis potent efficacy in gastrointestinal tumor inhibiton (inhibits MGC-803 (IC50=0.09 μM) and RKO (IC50=0.2 μM) cell lines) .
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Cat. No. |
Product Name |
Type |
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- HY-13631AG
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DX8951f (GMP)
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Fluorescent Dye
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Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
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Cat. No. |
Product Name |
Type |
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- HY-13631AG
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DX8951f (GMP)
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Biochemical Assay Reagents
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Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99843
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TROP2
ADC Antibody
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Cancer
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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 DNA topoisomerase I inhibitor Deruxtecan (HY-13631E) and Datopotamab .
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- HY-P99813
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HER3-DXd
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Antibody-Drug Conjugates (ADCs)
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Cancer
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Patritumab deruxtecan (HER3-DXd) is an antibody-drug conjugate (ADC) consisting of a fully human anti-HER3 IgG1 monoclonal antibody Patritumab (HY-P99275) attached to a topoisomerase I inhibitor payload via a tetrapeptide-based cleavable linker. Patritumab deruxtecan shows anticancer activity .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-16562S1
-
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Irinotecan-d10 (hydrochloride) is the deuterium labeled Irinotecan. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex[1][2].
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- HY-13631AS
-
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Exatecan-d5 (mesylate) is deuterium labeled Exatecan mesylate. Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL[1].
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- HY-13566AS
-
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Belotecan-d7 (hydrochloride) is the deuterium labeled Belotecan hydrochloride. Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative[1][2].
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-
-
- HY-13631DS
-
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Dxd-d5 is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) [1].
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-
-
- HY-16562S
-
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Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex[1].
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-
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- HY-121309S
-
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Doxorubicinone-d3 is the deuterium labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin[1]. Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
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- HY-126373S1
-
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SN-38 glucuronide- 13C6 is the 13C labeled SN-38 glucuronide (HY-126373) . SN-38 glucuronide is an inactive metabolite of the cancer agent Irinotecan. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
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-
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- HY-13704S
-
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SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively[1][2][3][4].
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-
- HY-13768S1
-
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Topotecan-d6 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95 μM of GSCs-U87[1][2].
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-
-
- HY-16560S
-
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Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) 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].
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Cat. No. |
Product Name |
Application |
Reactivity |
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- HY-P82492
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TOP1; DNA topoisomerase 1; DNA topoisomerase I
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WB, IHC-F, IHC-P, ICC/IF
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Human, Mouse, Rat |
Cat. No. |
Product Name |
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Classification |
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- HY-134723
-
|
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DBCO
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DBCO-PEG4-GGFG-Dxd is a agent-linker conjugate for ADC with potent antitumor activity by using Dxd (a DNA topoisomerase I 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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