Search Result
Results for "
Topoisomerase I inhibitor
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
24
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-16562
-
-
-
- HY-13631
-
|
DX-8951
|
ADC Payload
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.
|
-
-
- HY-13631A
-
|
DX8951f
|
ADC Payload
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.
|
-
-
- 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.
|
-
-
- HY-16562A
-
|
(+)-Irinotecan hydrochloride; CPT-11 hydrochloride; VAL-413
|
Topoisomerase
Autophagy
|
Cancer
|
|
Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer .
|
-
-
- 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 .
|
-
-
- HY-42487
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor with anticancer effects .
|
-
-
- HY-13566A
-
|
CKD-602
|
Topoisomerase
|
Cancer
|
|
Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative.
|
-
-
- HY-13555
-
-
-
- HY-156617A
-
|
SHR169265
|
ADC Payload
Topoisomerase
|
Cancer
|
(αR)-Cyclopropaneacetamide-Exatecan (SHR169265) is a DNA Topoisomerase I inhibitor with enhanced membrane permeability (with an IC50 of 1.34 μM against the human DNA Topoisomerase I). (αR)-Cyclopropaneacetamide-Exatecan exerts cytotoxic effects by inhibiting the enzymatic activity of Topoisomerase I, and this anticancer effect is independent of the expression level of HER2. (αR)-Cyclopropaneacetamide-Exatecan is an ADC Cytotoxin derived from Exatecan (HY-13631), which can be used in research related to advanced cancers such as breast cancer, gastric cancer, colorectal cancer and non-small cell lung cancer .
|
-
-
- HY-N6800A
-
-
-
- HY-B0063
-
|
ST1481
|
Topoisomerase
|
Cancer
|
|
Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity .
|
-
-
- HY-16228
-
|
|
Topoisomerase
|
Cancer
|
|
Genz-644282 is a non-camptothecin topoisomerase I inhibitor, used for cancer research.
|
-
-
- HY-N3488
-
|
|
Topoisomerase
Bacterial
Fungal
|
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 .
|
-
-
- HY-153795
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan is a bioactive drug-linker conjugate for ADC (Drug-Linker Conjugates for ADC). Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan consists of Exatecan (HY-13631) and a linker. Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan is applicable to ADC synthesis and cancer research. Exatecan acts as a DNA Topoisomerase I inhibitor .
|
-
-
- HY-14821
-
|
ST-1968
|
Topoisomerase
|
Cancer
|
|
Namitecan is a potent topoisomerase I inhibitor, with antitumor property.
|
-
-
- HY-13758A
-
|
BMS-247615 dihydrochloride
|
Topoisomerase
|
Cancer
|
|
TAS-103 dihydrochloride is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
|
-
-
- HY-100309
-
|
9-Amino-20(S)-camptothecin; 9-Amino-CPT
|
Topoisomerase
|
Cancer
|
|
9-Aminocamptothecin (9-Amino-CPT) is a topoisomerase I inhibitor with potent anticancer activity .
|
-
-
- HY-U00248A
-
|
MJ-III65 hydrochloride; NSC706744 hydrochloride
|
Topoisomerase
|
Cancer
|
|
LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity .
|
-
-
- HY-N6714
-
|
|
Topoisomerase
Androgen Receptor
Estrogen Receptor/ERR
Apoptosis
|
Infection
Cancer
|
|
Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
|
-
-
- HY-175203
-
-
-
- HY-148058
-
|
|
Topoisomerase
|
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 .
|
-
-
- HY-N0275
-
|
(±)-10-HCPT
|
Topoisomerase
|
Cancer
|
|
(±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.
|
-
-
- HY-U00248
-
|
MJ-III65; NSC706744
|
Topoisomerase
|
Cancer
|
|
LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity .
|
-
-
- HY-18350
-
|
LMP776
|
Topoisomerase
|
Cancer
|
|
Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities .
|
-
-
- HY-13618
-
|
J 107088; PF 804950
|
Topoisomerase
|
Cancer
|
|
Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM.
|
-
-
- 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 .
|
-
-
- HY-176976
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Exatecan-mpGNNG (Compound 10a) is the linker-payload component of an antibody-drug conjugate (ADC). Exatecan-mpGNNG is composed of Exatecan (HY-13631), a potent topoisomerase I inhibitor, and the linker .
|
-
-
- HY-159783
-
-
-
- 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 .
|
-
-
- HY-14812
-
|
Cositecan; BNP 1350
|
Topoisomerase
|
Cancer
|
|
Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity.
|
-
-
- HY-13670
-
|
GI147211; OSI-211
|
Topoisomerase
|
Cancer
|
|
Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects .
|
-
-
- HY-160774
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Val-Cit-PABC-DOX (compound 10109), an epsilon-poly-L-lysine-based drug conjugate, is an agent-linker conjugate for ADC by using a DNA topoisomerase I and topoisomerase II inhibitor, Doxorubicin (HY-15142), linked via the linker, Val-Cit-PABC .
|
-
-
- 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 .
|
-
-
- HY-13758
-
TAS-103
1 Publications Verification
BMS-247615
|
Topoisomerase
|
Cancer
|
|
TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
|
-
-
- HY-126142
-
-
-
- HY-19637
-
|
|
Topoisomerase
|
Cancer
|
|
SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
|
-
-
- HY-144774
-
|
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
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 .
|
-
-
- 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 .
|
-
-
- HY-19825
-
|
|
Topoisomerase
ADC Payload
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 .
|
-
-
- HY-13622A
-
|
BN 80927 free base
|
Topoisomerase
|
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 .
|
-
-
- HY-13622
-
|
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 .
|
-
-
- 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-162587
-
|
|
Topoisomerase
|
Cancer
|
|
Fagopyrine is a DNA topoisomerase I (Topo I) inhibitor. Fagopyrine is a photosensitizer that can be used in the study of tumors .
|
-
-
- HY-178373
-
|
|
Topoisomerase
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
MDM-2/p53
Caspase
|
Cancer
|
|
Topoisomerase I-IN-18, a derivative of Thiosemicarbazide (HY-Y0032), is a Topoisomerase I inhibitor. Topoisomerase I-IN-18 can disrupt DNA synthesis and transcription. Topoisomerase I-IN-18 inhibits tumor cell proliferation by inducing S-phase cell cycle arrest. Topoisomerase I-IN-18 can enhance mitochondria-mediated apoptosis, suppress cell migration, and increase intracellular Reactive Oxygen Species (ROS) levels. Topoisomerase I-IN-18 can increase p53 protein expression, γH2AX phosphorylation, upregulate Bax expression, downregulate Bcl-2 expression, and activate the caspase cascade. Topoisomerase I-IN-18 can be used for the study of lung cancer .
|
-
-
- HY-156969
-
|
|
Topoisomerase
Btk
|
Cancer
|
|
Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 11 can bind to BTK .
|
-
-
- 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 .
|
-
-
- HY-143266
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
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 .
|
-
-
- HY-161082
-
|
|
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 .
|
-
-
- HY-146437
-
|
|
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 .
|
-
- 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 .
|
-
- HY-168739
-
|
|
Topoisomerase
Reactive Oxygen Species (ROS)
Apoptosis
Survivin
Bcl-2 Family
IAP
DNA/RNA Synthesis
|
Cancer
|
|
Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-156464
-
|
|
Topoisomerase
|
Infection
|
|
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 .
|
-
- 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 .
|
-
- HY-169628
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II inhibitor 7 (Compound 5h) is a Topoisomerase I/II inhibitor .
|
-
- 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 .
|
-
- HY-146504
-
|
|
Topoisomerase
PI3K
Apoptosis
Reactive Oxygen Species (ROS)
|
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 .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-168632
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase I/II inhibitor 6 (compound 3i) is a potent inhibitor of topoisomerase I and II with IC50s of 4.77 and 15 µM, respectively. Topoisomerase I/II inhibitor 6 shows antiproliferative activities against human melanoma LOX IMVI cancer cell line with IC50 values of 26.7 and 25.4 µM, respectively. Topoisomerase I/II inhibitor 6 provokes substantial levels of early, late apoptosis and increases the expression level of active caspase-3 .
|
-
- HY-125930
-
|
|
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 .
|
-
- HY-175034
-
|
|
Topoisomerase
Apoptosis
MDM-2/p53
Bcl-2 Family
Caspase
|
Cancer
|
|
Topoisomerase I/II-IN-1 is a dual inhibitor of topoisomerase I/II. Topoisomerase I/II-IN-1 induces G2/M arrest and apoptosis in cancer cells by upregulating p53, p21, and Bax mRNA levels, caspase-3 protein levels, and the Bax/Bcl-2 ratio, while downregulating Bcl-2. Topoisomerase I/II-IN-1 is useful in the study of various cancers, including melanoma, renal cancer, colorectal cancer, and breast cancer .
|
-
- HY-169509
-
|
|
PARP
Necroptosis
Topoisomerase
RIP kinase
Mixed Lineage Kinase
|
Cancer
|
|
Topoisomerase I/II Inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of Topoisomerase I/II, capable of inducing DNA damage and PARP-1 activation, which subsequently leads to the activation of RIPK1, RIPK3, and MLKL, ultimately triggering necroptosis. Topoisomerase I/II Inhibitor 8 demonstrates remarkable anticancer activity by effectively targeting the nuclei of cancer cells and inducing cell death through necroptosis, showing great clinical potential in circumventing drug resistance in cancer treatment .
|
-
- HY-131540
-
|
BN 80245
|
Topoisomerase
|
Cancer
|
|
(±)-E-Homocamptothecin (BN 80245) is a topoisomerase I inhibitor. (±)-E-Homocamptothecin can be used for the research of cancer .
|
-
- HY-N6800
-
-
- HY-W713570
-
|
|
Topoisomerase
|
Cancer
|
|
Nectandrin B is an inhibitor of DNA topoisomerases I and II, which is found in Saururus chinensis. Nectandrin B is promising for research of cancers .
|
-
- HY-168150
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II inhibitor 5 (compund 1) simultaneously inhibits activities of TopoI and II by binding to and stabilizing the G4 structure .
|
-
- HY-W653896
-
|
|
Isotope-Labeled Compounds
Androgen Receptor
Apoptosis
Topoisomerase
Estrogen Receptor/ERR
|
Infection
|
|
Alternariol-d2 is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
|
-
- 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-122014
-
|
|
Topoisomerase
|
Others
|
|
39625 is a camptothecin ketone analogue, a stable, potent and selective topoisomerase I inhibitor, active against purified topoisomerase I and cytotoxic to cancer cells.
|
-
- HY-16562S
-
|
(+)-Irinotecan-d10; CPT-11-d10; VAL-413-d10free base
|
Topoisomerase
Autophagy
|
Cancer
|
|
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 .
|
-
- HY-125930A
-
|
|
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 .
|
-
- HY-N15319
-
|
Canangine
|
Topoisomerase
Fungal
|
Infection
|
|
Eupolauridine (Canangine) is a selective DNA topoisomerase II inhibitor with IC50 values of 20 μM for fungal topoisomerase I and 33 μM for human topoisomerase I. Eupolauridine exerts antifungal activity by inhibiting the catalytic activity of topoisomerase II and stabilizing its cleavage complex with DNA, leading to DNA damage. Eupolauridine is promising for research of fungal infectious diseases .
|
-
- HY-16562R
-
|
(+)-Irinotecan (Standard); CPT-11 (Standard); VAL-413free base (Standard)
|
Reference Standards
Topoisomerase
Autophagy
|
Cancer
|
|
Irinotecan (Standard) is the analytical standard of Irinotecan. This product is intended for research and analytical applications. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
|
-
- HY-N10115
-
-
- HY-18350A
-
|
LMP776 hydrochloride
|
Topoisomerase
|
Cancer
|
|
Indimitecan hydrochloride is a topoisomerase I (Top1) inhibitor with anticancer activities .
|
-
- 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-13622B
-
|
BN 80927 TFA
|
Topoisomerase
|
Cancer
|
|
Elomotecan TFA is a potent inhibitor of topoisomerases I and II. Elomotecan TFA is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan TFA reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II .
|
-
- HY-13670A
-
|
GI147211 dihydrochloride; OSI-211 dihydrochloride
|
Topoisomerase
|
Cancer
|
|
Lurtotecan dihydrochloride (GI147211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan dihydrochloride has anticancer effects .
|
-
- HY-13565
-
|
NSC 655649; BMS 181176; BMY 27557
|
Topoisomerase
|
Cancer
|
|
Becatecarin is a rebeccamycin analog with antitumor effects. Becatecarin intercalates into DNA and inhibites the catalytic activity of topoisomerases I/II.
|
-
- HY-W897655
-
|
O-Acetylcamptothecin
|
Topoisomerase
|
Others
|
|
20-O-Acetylcamptothecin (O-Acetylcamptothecin) is a derivative of Camptothecin (HY-16560) and an inhibitor of Topoisomerase I .
|
-
- HY-120185
-
|
UCT-1003
|
Topoisomerase
|
Infection
Cancer
|
|
Saintopin is an antitumor antibiotic. Saintopin is also an inhibitor of DNA topoisomerases I and II. Saintopin induces DNA cleavage .
|
-
- HY-N10367
-
|
|
Topoisomerase
|
Cancer
|
|
Corydamine, 3-arylisoquinoline alkaloid, is a potent DNA topoisomerase I/II inhibitor. Corydamine has anti-cancer activity .
|
-
- HY-13768AR
-
|
SKF 104864A hydrochloride (Standard); NSC 609669 hydrochloride (Standard)
|
Reference Standards
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
|
Topotecan (hydrochloride) (Standard) is the analytical standard of Topotecan (hydrochloride). This product is intended for research and analytical applications. Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.
|
-
- HY-179018
-
|
|
Topoisomerase
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
Topoisomerase II-IN-25 (Compound 6a) is a selective inhibitor of topoisomerase II and has no inhibitory activity on topoisomerase I. Topoisomerase II-IN-25 exhibits significant anti-PC-3 cell activity. Topoisomerase II-IN-25 significantly increases intracellular ROS levels, inducing oxidative stress. Topoisomerase II-IN-25 causes depolarization of mitochondrial membrane potential and promotes cell apoptosis. Topoisomerase II-IN-25 blocks PC-3 cells in the G2/M phase. Topoisomerase II-IN-25 can be used for the study of prostate cancer .
|
-
- HY-N6714R
-
|
|
Reference Standards
Topoisomerase
Androgen Receptor
Estrogen Receptor/ERR
Apoptosis
|
Infection
Cancer
|
|
Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
|
-
- HY-181725
-
|
|
Topoisomerase
Apoptosis
MDM-2/p53
Caspase
Bcl-2 Family
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Topoisomerase I-IN-20 is a Topoisomerase I inhibitor. Topoisomerase I-IN-20 disrupts DNA synthesis and transcription, thereby inhibiting the proliferation and migration of cancer cells. Topoisomerase I-IN-20 induces S-phase cell cycle arrest and mitochondria-mediated Apoptosis in cancer cells, which is characterized by upregulated expression of p53, Bax, caspase-3 and caspase-9, along with downregulated expression of Bcl-2. Topoisomerase I-IN-20 increases intracellular ROS levels. Topoisomerase I-IN-20 is applicable to lung cancer-related research .
|
-
- HY-164380
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
MC-Val-Cit-Gly-exatecan-β-D-glucopyranosiduronic acid (example 13) is a drug-linker conjugate that consists of a DNA topoisomerase I inhibitor Exatecan (HY-13631) and a linker (HY-180841). MC-Val-Cit-Gly-exatecan-β-D-glucopyranosiduronic acid can be used in synthesis of ADC .
|
-
- HY-203913
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I-IN-19 (Example 36) is a Topoisomerase I inhibitor. Topoisomerase I-IN-19 can be used to investigate Topoisomerase I-mediated diseases such as cancer .
|
-
- HY-182816
-
|
|
Topoisomerase
DNA/RNA Synthesis
Bacterial
|
Infection
|
|
Topoisomerase I-IN-22 is an inhibitor of MRSA DNA Topoisomerase I with an IC50 of 0.85 μg/mL. Topoisomerase I-IN-22 can specifically disrupt the cell membrane structure of MRSA, enter the interior of bacteria and inhibit the activity of DNA Topoisomerase I, thereby interfering with the processes of DNA replication and transcription. Topoisomerase I-IN-22 can be used for the research of MRSA infection .
|
-
- HY-185279
-
|
HS-20093; GSK5764227
|
Antibody-Drug Conjugates (ADCs)
CD276/B7-H3
|
Cancer
|
|
Risvutatug rezetecan (HS-20093; GSK5764227) is a B7-H3-targeting antibody-drug conjugate (ADC). Risvutatug rezetecan binds to B7-H3 on tumor cells and delivers a topoisomerase I inhibitor payload via a tumor microenvironment-responsive cleavable linker. Risvutatug rezetecan is applicable for the research of extensive-stage small cell lung cancer and non-small cell lung cancer .
|
-
- HY-182758
-
|
|
Topoisomerase
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Topoisomerase I-IN-21 is a promising topoisomerase I inhibitor with an IC50 of 18.79 μM. Topoisomerase I-IN-21 shows higher selectivity toward cancer cells over normal CD8 + cells. Topoisomerase I-IN-21 induces G0/G1 cell cycle arrest and apoptosis. Topoisomerase I-IN-21 activates the cGAS-STING pathway, leading to enhanced immune gene expression. Topoisomerase I-IN-21 can be used for research on leukemia, non-small-cell lung, colon, central nervous system, melanoma, ovarian, renal, prostate, and breast cancers .
|
-
- HY-N2062
-
|
|
Topoisomerase
|
Cancer
|
|
10-Nitrocamptothecin is a topoisomerase I inhibitor with an IC50 of 0.64 μM. 10-Nitrocamptothecin interferes with the formation of cleavable complexes, thereby inhibiting the activity of Topoisomerase I. 10-Nitrocamptothecin is applicable for cancer research .
|
-
- HY-182926
-
|
|
DNA/RNA Synthesis
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II-IN-9 is a topoisomerase I/II inhibitor (IC50<10 μM) and a DNA damage inducer. Topoisomerase I/II-IN-9 blocks the interaction between the enzyme and DNA by binding to the DNA-binding pocket of the enzyme. Topoisomerase I/II-IN-9 activates the cGAS-STING pathway and promotes the accumulation of cytoplasmic double-stranded DNA. This further drives the production of type I interferons, CCL5, CXCL10 and interferon-stimulated genes, and induces anti-tumor immune responses in vivo. Topoisomerase I/II-IN-9 can be applied to the research of related diseases such as triple-negative breast cancer, colorectal cancer and gastric cancer .
|
-
- HY-16562S2
-
-
- HY-N4329
-
|
|
Topoisomerase
|
Others
|
|
Nidulalin A is a DNA topoisomerase II inhibitor with an IC50 of 2.2 μM. Nidulalin A has an IC50 of 172 μM for DNA topoisomerase I. Nidulalin A has certain cytotoxicity .
|
-
- HY-182748
-
|
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
NL-26 is a Topoisomerase I inhibitor. NL-26 stabilizes the covalent Topoisomerase I (Topo I)-DNA complex, prevents DNA religation and triggers the DNA damage response. NL-26 induces G2/M cell cycle arrest and apoptosis in cancer cells. NL-26 can be used for the research of colorectal cancer .
|
-
- HY-180509
-
|
|
Topoisomerase
MDM-2/p53
|
Cancer
|
|
Topoisomerase I/IIα-IN-1 (Compound 20i) is a Topoisomerase I/IIα inhibitor. MDM2-IN-27 can effectively block the inhibitory effect of MDM2 on p53, thereby activating the p53 pathway. MDM2-IN-27 has relatively poor anti-proliferative activity against breast cancer, colon cancer, and cutaneous squamous cell carcinoma .
|
-
- HY-164789
-
|
SKB264; MK-2870
|
Antibody-Drug Conjugates (ADCs)
TROP2
|
Cancer
|
|
Sacituzumab tirumotecan is an antibody-drug conjugate and TROP2-directed, topoisomerase I inhibitor payload-delivering agent, with a TROP2 EC50 of 2.787 ng/ml, TROP2 Ka of 0.3083 nM, and topoisomerase I IC50 of 0.7 μmol/L. Sacituzumab tirumotecan can be used for the research of metastatic triple-negative breast cancer, and metastatic non-small cell lung cancer .
|
-
- HY-183330
-
|
|
Topoisomerase
Reactive Oxygen Species (ROS)
Apoptosis
MDM-2/p53
Caspase
Bcl-2 Family
|
Cancer
|
|
Topo I/II-IN-3 is a dual inhibitor of topoisomerase I/II (topoisomerase I/II), with an IC50 of 8.99 μM against Topo I and an IC50 of 26.92 μM against Topo II. Topo I/II-IN-3 induces DNA damage, elevates intracellular ROS levels, activates the mitochondrial apoptosis pathway, and exerts cytotoxicity against cancer cells. Topo I/II-IN-3 upregulates the expression of γ-H2AX, p53, activated caspase-9, Bax and activated caspase-3, while downregulating the expression of Bcl-2. Topo I/II-IN-3 can be used in research related to breast cancer, liver cancer and gastric cancer .
|
-
- HY-13631U
-
|
DX-8951 hydrochloride
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan (DX-8951) hydrochloride 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-16568R
-
|
(+)-Irinotecan hydrochloride trihydrate (Standard); CPT-11 hydrochloride trihydrate (Standard)
|
Reference Standards
Topoisomerase
Autophagy
|
Cancer
|
|
Irinotecan (hydrochloride trihydrate) (Standard) is the analytical standard of Irinotecan (hydrochloride trihydrate). This product is intended for research and analytical applications. Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate) is a topoisomerase I inhibitor with antitumor activity .
|
-
- HY-13631P
-
|
DX-8951 mesylate dihydrate
|
ADC Payload
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 .
|
-
- HY-181697
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
SDP-LIV1 drug-linker is a drug-linker conjugate formed by the condensation of a linker and a topoisomerase I inhibitor. It can be used for the preparation of ADCs, such as SDP-LIV1.
|
-
- HY-16562AR
-
|
(+)-Irinotecan hydrochloride (Standard); CPT-11 hydrochloride (Standard); VAL-413 (Standard)
|
Reference Standards
Topoisomerase
Autophagy
|
Cancer
|
|
Irinotecan (hydrochloride) (Standard) is the analytical standard of Irinotecan (hydrochloride). This product is intended for research and analytical applications. Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer .
|
-
- HY-16562AS
-
|
(+)-Irinotecan-d5 (hydrochloride; CPT-11-d5 hydrochloride; VAL-413-d5
|
Autophagy
Topoisomerase
Isotope-Labeled Compounds
|
Cancer
|
|
Irinotecan-d5 hydrochloride is deuterated labeled Irinotecan hydrochloride (HY-16562A). Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer .
|
-
- HY-16472R
-
|
|
Reference Standards
Antibiotic
Bacterial
|
Infection
|
|
Irinotecan (hydrochloride) (Standard) is the analytical standard of Irinotecan (hydrochloride). This product is intended for research and analytical applications. Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer .
|
-
- HY-185370
-
|
Pegylated liposomal doxorubicin; Liposomal doxorubicin; Doxorubicin hydrochloride liposome
|
Liposome
Topoisomerase
Antibiotic
|
Cancer
|
|
Doxorubicin liposome is a liposome-encapsulated form of doxorubicin hydrochloride (HY-15142). Doxorubicin hydrochloride, a cytotoxic anthracycline antibiotic, is a potent human DNA topoisomerase I and topoisomerase II inhibitor. Compared to traditional doxorubicin, liposome encapsulation reduces its cardiotoxicity and prolongs its circulation time, thus enabling it to effectively target tumor tissue.
|
-
- 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-171689
-
|
AZD 8205; P-Sam
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
|
Puxitatug samrotecan (AZD 8205) is a B7-H4-directed antibody-drug conjugate (ADC) bearing a Topoisomerase I inhibitor (TOP1i) payload. Puxitatug samrotecan improves HR +/HER2 - breast cancer .
|
-
- 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-100777
-
|
|
Topoisomerase
|
Neurological Disease
Cancer
|
|
DACA (XR 5000) is a potential and blood-brain barrier-penetrating topoisomerase I and II inhibitor. DACA can be used in the research of colorectal cancer, leukemia and lung cancer .
|
-
- HY-177585
-
|
BLD1102
|
ADC Payload
Topoisomerase
|
Cancer
|
|
BCPT02 (BLD1102) is a Topoisomerase-I inhibitor and ADC payload (ADC Payload). BCPT02 can form the ADC BCG041. BCPT02 is applicable to cancer-related research .
|
-
- 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-13631D
-
|
Exatecan derivative for ADC
|
Topoisomerase
ADC Payload
|
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-156848
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Fmoc-GGFG-DXd is a drug-linker conjugate for ADC. Fmoc-GGFG-DXd contains a ADC linker Fmoc-GGFG and a DNA topoisomerase I inhibitor DXd (HY-13631D) .
|
-
- HY-185371
-
|
Irinotecan hydrochlorid liposomee; Liposomal irinotecan
|
Liposome
Topoisomerase
|
Cancer
|
|
Irinotecan liposome is a liposome-encapsulated form of Irinotecan hydrochlorid (HY-16562A) (a topoisomerase I inhibitor). Compared with Irinotecan, Irinotecan liposome enhances antitumor activity, reduces drug release rate, and avoids neutropenia.
|
-
- 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) .
|
-
- 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-164836
-
-
- HY-15142A
-
-
- HY-15142
-
|
Hydroxydaunorubicin hydrochloride; ADR
|
Topoisomerase
ADC Payload
AMPK
Autophagy
Apoptosis
HIV
HBV
Mitophagy
Antibiotic
Bacterial
Fluorescent Dye
|
Infection
Cancer
|
|
Doxorubicin hydrochloride (Hydroxydaunorubicin hydrochloride; ADR), 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-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-13631AS1
-
-
- 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-13631G
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan analog 13 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-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-147408
-
|
SHR9265
|
Topoisomerase
ADC Payload
|
Cancer
|
|
Rezetecan (SHR9265) is a topoisomerase I inhibitor. In addition, Rezetecan can be used to synthesize Trastuzumab rezetecan, an antineoplastic agent. Rezetecán can be used as a cytotoxic payload (ADC Cytotoxin) in antibody-drug conjugates (ADCs) .
|
-
- HY-49556
-
|
|
Topoisomerase
|
Cancer
|
|
(S)-Benzyl 2-cyclopropyl-2-hydroxyacetate is an intermediate reactant in the synthesis of Camptothecin (HY-16560). Camptothecin is an inhibitor of the DNA topoisomerase Topo I, withIC50=679 nM .
|
-
- HY-N0275R
-
|
(±)-10-HCPT (Standard)
|
Topoisomerase
Reference Standards
|
Cancer
|
|
(±)-10-Hydroxycamptothecin (Standard) is the analytical standard of (±)-10-Hydroxycamptothecin. This product is intended for research and analytical applications. (±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.
|
-
- 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-N2306
-
|
Aclarubicin
|
Topoisomerase
DNA/RNA Synthesis
Proteasome
Antibiotic
|
Cancer
|
|
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-161970
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
XSJ05 is a camptothecin (CPT) derivative that can inhibit topoisomerase I (Topo I) to exert anti-cancer activity. XSJ05 can trigger DNA double-strand breaks, leading to DNA damage. XSJ05 can inhibit the growth of colorectal cancer (CRC), arrest the cell cycle in G2/M phase, and induce apoptosis .
|
-
- HY-148668A
-
-
- HY-13631R
-
|
DX-8951 (Standard)
|
ADC Payload
Reference Standards
Topoisomerase
|
Cancer
|
|
Exatecan (Standard) is the analytical standard of Exatecan. This product is intended for research and analytical applications. 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.
|
-
- HY-160788
-
-
- 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-48878
-
|
|
ADC Payload
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-177548
-
-
- HY-13631AG
-
|
DX8951f
|
ADC Payload
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 .
|
-
- HY-164647
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Val-Ala-PABC-N(Mesylpropane)-Exatecan is an agent-linker conjugate for ADC. Val-Ala-PABC-N(Mesylpropane)-Exatecan is a Exatecan (a DNA topoisomerase I inhibitor) d with cleavable Val-Ala-PABC-N(Mesylpropane) linker .
|
-
- 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-164835
-
|
SMP-54418
|
Drug-Linker Conjugates for ADC
Microtubule/Tubulin
Topoisomerase
|
Cancer
|
|
VcMMAE-Deruxtecan (SMP-54418) is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule MMAE (HY-15162) (Microtubule inhibitor) and Exatecan (HY-13631) (DNA topoisomerase I inhibitor). VcMMAE-Deruxtecan can be used for ADC synthesis.
|
-
- HY-A0210
-
-
- HY-49861
-
|
|
ADC Payload
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 Payload
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-400316
-
|
|
ADC Payload
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-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-43565
-
|
|
ADC Payload
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-13631DS
-
|
Exatecan-d5 derivative for ADC
|
Topoisomerase
ADC Payload
|
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) .
|
-
- HY-42487S1
-
|
|
Isotope-Labeled Compounds
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan Intermediate 1-d2 is the deuterium labeled Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor with anticancer effects.
|
-
- HY-126373
-
|
SN-38G
|
Drug Metabolite
|
Cancer
|
|
SN-38 glucuronide is an inactive metabolite of the anticancer active molecule Irinotecan (HY-16562) and has toxic effects on the gastrointestinal tract. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
|
-
- 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-W665464
-
|
|
Drug Derivative
Topoisomerase
|
Cancer
|
|
(Rac)-7-Ethyl-10-hydroxycamptothecin is the derivative of (±)-10-Hydroxycamptothecin (HY-N0275). (±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity .
|
-
- HY-N8250
-
|
|
Topoisomerase
PEPCK
|
Metabolic Disease
|
|
cis-THSG is a selective and orally active DNA topoisomerase II inhibitor with no activity against DNA topoisomerase I. cis-THSG suppresses transcription of PEPCK. cis-THSG reduces blood glucose levels, ameliorates glucose intolerance, and alleviates insulin resistance in high fat diet-induced diabetic male CF-1 mice. cis-THSG can be used for the research of type 2 diabetes mellitus .
|
-
- HY-158230
-
|
|
Topoisomerase
|
Cancer
|
|
SN-398 is a derivative of Camptothecin (HY-158230), which is an antitumor drug. Acting by inhibiting mammalian DNA topoisomerase I (Topo I), stabilizing the Topo I-DNA complex prevents DNA rewiring to induce Topo I mediated DNA breaks. In Hela cell tests, SN-398 shows stronger antitumor activity than SN-38 (HY-13704) (IC50=1.562 μM). SN-398 can be used to study the anti-proliferation and growth inhibition of Topo I in cancer cells .
|
-
- 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-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-120638
-
|
|
Topoisomerase
|
Cancer
|
|
BMS-250749 is a topoisomerase I (Top I) inhibitor of the fluoroglycosyl-3,9-difluoroindolecarbazole class. BMS-250749 exhibits potent cytotoxicity and selectivity, and shows curative antitumor activity against Lewis lung cancer. BMS-250749 exhibits broad-spectrum antitumor activity superior to CPT-11 in certain preclinical xenograft models. .
|
-
- 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-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-10529
-
-
- 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 .
|
-
- HY-161628
-
|
|
Topoisomerase
|
Cancer
|
|
Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model .
|
-
- HY-148819
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
NH2-bicyclopentane-7-MAD-MDCPT (Formula I) is a topoisomerase I (TOP1) inhibitor. NH2-bicyclopentane-7-MAD-MDCPT is applicable to the synthesis of the ADC ABBV-969. NH2-bicyclopentane-7-MAD-MDCPT is used in research on lung adenocarcinoma and melanoma .
|
-
![NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT](//file.medchemexpress.com/product_pic/hy-148819.gif)
- HY-148819A
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
NH2-bicyclopentane-7-MAD-MDCPT hydrochloride (Formula I) is a topoisomerase I (TOP1) inhibitor. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is applicable to the synthesis of the ADC ABBV-969. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is used in research on lung adenocarcinoma and melanoma .
|
-
![NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride](//file.medchemexpress.com/product_pic/hy-148819a.gif)
- HY-174151
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
XSJ110 is a potent irreversible topoisomerase I (Topo I) inhibitor with an IC50 value of 0.133 μM. XSJ110 blocks DNA topoisomerization, induces DNA double-strand breaks, and triggers cell cycle arrest at G0/G1 phase, inducing tumor cell apoptosis. XSJ110 is promising for research of ampullary carcinoma (AC) .
|
-
- HY-16560
-
|
Campathecin; (S)-(+)-Camptothecin; CPT
|
Topoisomerase
ADC Payload
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-42487R
-
|
|
ADC Payload
Reference Standards
Topoisomerase
|
Cancer
|
|
Exatecan Intermediate 1 (Standard) is the analytical standard of Exatecan Intermediate 1. This product is intended for research and analytical applications. Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor with anticancer effects .
|
-
- HY-122481
-
|
|
Topoisomerase
Apoptosis
Bcl-2 Family
Cytochrome P450
|
Cancer
|
|
Thaspine acetate, an alkaloid, is a topoisomerase I and II inhibitor. Thaspine acetate induces cancer cell apoptosis. Thaspine acetate induces Bak and Bax activation, mitochondrial cytochrome c release and mitochondrial membrane permeabilization. Thaspine acetate can be isoalted from the cortex of the South American tree Croton lechleri .
|
-
- HY-143692
-
-
- HY-171931
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Aminocaproyl-Val-Cit-PABC-Exatecan is a drug-linker conjugate for ADC, consiting of a cleavable linker (Aminocaproyl-Val-Cit-PABC) and Exatecan (HY-13631) (topoisomerase I inhibitor). Aminocaproyl-Val-Cit-PABC-Exatecan can be used for ADC molecues synthesis .
|
-
- 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-13555R
-
-
- HY-15142R
-
|
Hydroxydaunorubicin hydrochloride (Standard); ADR (Standard)
|
Reference Standards
Topoisomerase
ADC Payload
AMPK
Autophagy
Apoptosis
HIV
HBV
Mitophagy
Antibiotic
Bacterial
Fluorescent Dye
|
Infection
Cancer
|
|
Doxorubicin hydrochloride (Standard) is the analytical standard of Doxorubicin hydrochloride. This product is intended for research and analytical applications. 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-163487
-
|
AZD8205 drug-linker
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Puxitatug samrotecan drug-linker (AZD8205 drug-linker) is a drug-linker conjugate for ADC, which comprises a topoisomerase I inhibitor and a linker. Puxitatug samrotecan drug-linker can be used to synthesis antibody-drug conjugate (ADC), Puxitatug samrotecan (HY-171689) .
|
-
- HY-173243
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Val-Ala-PAB-SN38 is a drug-linker conjugate for ADC, composed of ADC linker Val-Ala-PAB (HY-125933) and SN38 (HY-13704), which is the active metabolite of the Topoisomerase I inhibitor Irinotecan (HY-16562) .
|
-
- HY-13631M
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Gly-Gly-Phe-Gly-NH-O-CO-Exatecan is a Drug-Linker Conjugates for ADC, consiting of an ADC linker and Exatecan (HY-13631) (topoisomerase I inhibitor). Gly-Gly-Phe-Gly-NH-O-CO-Exatecan can be used for ADC molecues synthesis.
|
-
- HY-18351A
-
|
LMP-400 hydrochloride; NSC-724998 hydrochloride
|
Topoisomerase
|
Infection
Cancer
|
|
Indotecan hydrochloride, 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 hydrochloride prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
|
-
- HY-148668
-
|
SHR-A1811 Drug-linker
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan (SHR-A1811 Drug-linker) is a agent-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNA Topoisomerase I inhibitor (IC50=2.2 μM) .
|
-
- HY-173243A
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Val-Ala-PAB-SN38 TFA is a drug-linker conjugate for ADC, composed of ADC linker Val-Ala-PAB (HY-125933) and SN38 (HY-13704), which is the active metabolite of the Topoisomerase I inhibitor Irinotecan (HY-16562) .
|
-
- HY-177546
-
-
- HY-171931A
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Aminocaproyl-Val-Cit-PABC-Exatecan TFA is a drug-linker conjugate for ADC, consiting of a cleavable linker (Aminocaproyl-Val-Cit-PABC) and Exatecan (HY-13631) (topoisomerase I inhibitor). Aminocaproyl-Val-Cit-PABC-Exatecan TFA can be used for ADC molecues synthesis .
|
-
- HY-13631AS
-
|
DX8951f-d5; Deuterated labeled Exatecan mesylate
|
Isotope-Labeled Compounds
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan-d5 (DX8951f-d5) mesylate is deuterium labeled Exatecan mesylate (HY-13631A). Exatecan mesylate 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 .
|
-
- HY-125331
-
|
|
Topoisomerase
ADC Payload
|
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-43565C
-
|
|
Drug Intermediate
|
Cancer
|
|
(1S,9R)-Ac-Exatecan 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-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-100777R
-
|
|
Topoisomerase
Reference Standards
|
Cancer
|
|
DACA (Standard) is the analytical standard of DACA (HY-100777). This product is intended for research and analytical applications. DACA (XR 5000) is a blood-brain barrier-penetrating topoisomerase I and II inhibitor. DACA can be used in the research of colorectal cancer, leukemia and lung cancer .
|
-
- HY-156686
-
|
|
ADC Payload
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-128994
-
|
|
Drug Intermediate
|
Cancer
|
|
GGFG-Exatecan is a synthetic intermediate for drug-linker conjugates used in antibody-drug conjugates (ADCs). GGFG-Exatecan consists of a glycyl-glycyl-phenylalanyl-glycine (GGFG) tetrapeptide linker and a DNA topoisomerase I inhibitor Exatecan (HY-13631). GGFG-Exatecan can be used for the study of cancer .
|
-
- 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 (HY-13631) (topoisomerase I inhibitor). Val-Ala-PABC-Exatecan can be used for ADC molecues synthesis, such as Mal-PEGn-amide-va-Exatecan .
|
-
- 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-N2306R
-
|
Aclarubicin (Standard)
|
Reference Standards
Topoisomerase
DNA/RNA Synthesis
Proteasome
Antibiotic
|
Cancer
|
|
Aclacinomycin A (Standard) is the analytical standard of Aclacinomycin A. This product is intended for research and analytical applications. 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-136170
-
MC-SN38
2 Publications Verification
|
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-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-13566R
-
|
CKD-602 free base (Standard)
|
Topoisomerase
Apoptosis
Reference Standards
|
Cancer
|
|
Belotecan (Standard) is the analytical standard of Belotecan. This product is intended for research and analytical applications. 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-46081
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
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-43564
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
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-13631N
-
|
(9R)-DX8951f
|
Drug Derivative
ADC Payload
Topoisomerase
|
Cancer
|
|
(9R)-Exatecan (DX8951f) is the (1R,9S) stereoisomer of Exatecan (HY-13631). 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.
|
-
- 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-44369
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
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-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-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-164792
-
-
- 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-45157
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
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-N15249
-
|
Isovalerylspiramycin I; Shengjimycin E
|
Topoisomerase
DNA/RNA Synthesis
Checkpoint Kinase (Chk)
Apoptosis
Bacterial
|
Infection
Cancer
|
|
4"-Isovalerylspiramycin I (Isovalerylspiramycin I) is a topoisomerase 1 (TOP1) inhibitor and an antitumor agent. 4"-Isovalerylspiramycin I directly binds to TOP1, suppresses DNA replication, and induces DNA damage. 4"-Isovalerylspiramycin I downregulates phosphorylated CHEK1 and the ATR/CHEK1 DNA damage repair pathway, blocks DNA repair, and augments DNA damage. 4"-Isovalerylspiramycin I suppresses proliferation, migration, and invasion of osteosarcoma cells. 4"-Isovalerylspiramycin I induces apoptosis and cell cycle arrest in osteosarcoma cells. 4"-Isovalerylspiramycin I exerts antibacterial activity against methicillin-resistant Staphylococcus aureus. 4"-Isovalerylspiramycin I can be used for the research of osteosarcoma, upper respiratory bacterial infections, and methicillin-resistant Staphylococcus aureus infection .
|
-
- HY-N5038
-
|
|
Topoisomerase
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
|
Mauritianin is an orally active kaempferol glycoside. Mauritianin can be isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor. Mauritianin has hepatoprotective, neuroprotective, and renoprotective activities. Mauritianin increases vascular tone when used in combination with Alcesefoliside (HY-N5049) .
|
-
- 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-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 an antibody agent conjugate (ADC), ABBV-969 .
|
-
![Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT](//file.medchemexpress.com/product_pic/hy-148820.gif)
- HY-13704S
-
|
NK012-d3
|
Topoisomerase
ADC Payload
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 .
|
-
- HY-13704
-
|
7-Ethyl-10-hydroxycamptothecin
|
Drug Metabolite
Topoisomerase
ADC Payload
Autophagy
|
Infection
Cancer
|
|
SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 can bind to RPL15. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254) .
|
-
- HY-168285
-
-
- HY-P10765
-
|
|
Peptide-Drug Conjugates (PDCs)
Topoisomerase
|
Cancer
|
|
DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer .
|
-
- HY-128994A
-
|
|
Drug Intermediate
|
Cancer
|
|
GGFG-Exatecan TFA is a synthetic intermediate for drug-linker conjugates used in antibody-drug conjugates (ADCs). GGFG-Exatecan TFA consists of a glycyl-glycyl-phenylalanyl-glycine (GGFG) tetrapeptide linker and a DNA topoisomerase I inhibitor Exatecan (HY-13631). GGFG-Exatecan TFA can be used for the study of 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-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-159483
-
|
|
Topoisomerase
Autophagy
Glutathione Peroxidase
|
Cancer
|
|
SelB-1 serves as a dual inhibitor for Topoisomerase I/II. SelB-1 possesses anticancer activity and can be utilized in the research of prostate cancer and colon cancer. Furthermore, SelB-1 is also capable of inducing autophagy gene expression and lipid peroxidation, while simultaneously reducing the level of GSH .
|
-
- HY-16560S
-
|
Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5
|
Isotope-Labeled Compounds
Topoisomerase
ADC Payload
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 . 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-P992124
-
|
BAT8006 Antibody; BAT-6028
|
Folate Receptor (FR)
|
Cancer
|
|
Onvontatug (BAT8006 Antibody) is a humanized monoclonal antibody targeting folate receptor α (FRα). Onvontatug can be used to construct antibody-drug conjugates (ADCs), such as BAT8006. It is applicable to research related to platinum-resistant ovarian cancer .
|
-
- HY-10529R
-
-
- HY-W008874
-
|
|
Topoisomerase
|
Cancer
|
|
meso-Tetra(4-pyridyl)porphine (Compound 10) is a porphyrin derivative. meso-Tetra(4-pyridyl)porphine is a weak inhibitor of human topoisomerase I (Top1) with an EC50 value greater than 50 µM. meso-Tetra(4-pyridyl)porphine can be used in tumor research .
|
-
- 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-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-13631T
-
|
(1R,9S)-DX8951f
|
Drug Derivative
ADC Payload
Topoisomerase
|
Cancer
|
|
(1R,9S)-Exatecan (DX8951f) is the (1R,9S) stereoisomer of Exatecan (HY-13631). 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 .
|
-
- HY-122532
-
|
|
Histone Methyltransferase
|
Cancer
|
|
Fagaronine chloride is an alkaloid with inhibitory activity against reverse transcriptase and topoisomerase I. Fagaronine chloride can effectively inhibit the reverse transcriptase of RSii tumor virus at a concentration of 6-60 μg/mL. Fagaronine chloride rapidly blocks the synthesis of DNA polymerase by interacting with the template primer. Fagaronine chloride has shown anti-tumor potential, especially in the study of retroviral infection .
|
-
- HY-P992130
-
|
TQB2102 Antibody
|
ADC Antibody
EGFR
|
Cancer
|
|
Rolditamig (TQB2102 Antibody) is a recombinant humanized anti-human epidermal growth factor receptor 2 (HER2) antibody. Rolditamig can be conjugated with an enzyme-cleavable linker and a topoisomerase I inhibitor to form the ADC TQB2102. Rolditamig is applicable to research on solid tumors such as HER2-positive breast cancer .
|
-
- HY-P99813
-
|
HER3-DXd; U3-1402
|
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-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-171580
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Mc-PEG4-Val-Ala-PAB-Exatecan is a Drug-linker conjugate for ADC. Mc-PEG4-Val-Ala-PAB-Exatecan contains the ADC linker (Mc-PEG4-Val-Ala-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631) .
|
-
- HY-B1099R
-
|
|
DNA/RNA Synthesis
Topoisomerase
Parasite
Reference Standards
|
Infection
|
|
Hycanthone (Standard) is the analytical standard of Hycanthone. This product is intended for research and analytical applications. 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-181836
-
|
|
IKK
Topoisomerase
Apoptosis
NF-κB
Reactive Oxygen Species (ROS)
Bcl-2 Family
|
Cancer
|
|
IKKβ-IN-6 is an antitumor agent. IKKβ-IN-6 inhibits IKKβ (IC50: 18.24 μM), thereby suppressing the phosphorylation of p65 and IκBα, blocking the nuclear translocation of p65, and subsequently regulating genes controlled by NF-κB. IKKβ-IN-6 also targets topoisomerase I (Topo I), induces DNA damage, ROS accumulation, loss of mitochondrial membrane potential, and S-phase arrest. IKKβ-IN-6 is applicable to related research on colorectal cancer .
|
-
- HY-180508
-
|
|
MDM-2/p53
Topoisomerase
|
Cancer
|
|
MDM2-IN-27 (Compound 20k) is an MDM2 inhibitor. MDM2-IN-27 can effectively block the inhibitory effect of MDM2 on p53, thereby activating the p53 pathway. MDM2-IN-27 has a certain topoisomerase I inhibitory activity and has a very weak inhibitory effect on topoisomerase IIα. MDM2-IN-27 exhibits significant anti-proliferative activity against breast cancer, colon cancer, and cutaneous squamous cell carcinoma .
|
-
- HY-16560R
-
|
Campathecin (Standard); (S)-(+)-Camptothecin (Standard); CPT (Standard)
|
Reference Standards
Topoisomerase
ADC Payload
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Infection
Cancer
|
|
Camptothecin (Standard) (Campathecin (Standard)) is the analytical standard of Camptothecin (HY-16560). This product is intended for research and analytical applications. 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-132561S
-
|
APC-d3
|
Isotope-Labeled Compounds
Topoisomerase
Cholinesterase (ChE)
|
Cancer
|
|
RPR121056-d3 is the deuterium labeled RPR121056. RPR121056 is a metabolite of Irinotecan (HY-16562), 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 study of colorectal cancer. Irinotecan also directly inhibits AChE .
|
-
- HY-79490
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Ac-Exatecan is acetylation-modified Exatecan (HY-13631). Exatecan is a common toxin component in ADC preparation (ADC cytotoxin) and an inhibitor of DNA topoisomerase I (IC50 = 2.2 μM). Exatecan has antitumor activity. Exatecan can be used as a payload for ADC. Exatecan is effective against P-glycoprotein mediated multi-drug resistant cells .
|
-
- HY-W046353
-
|
o-Methoxycinnamaldehyde
|
Apoptosis
NF-κB
Topoisomerase
Mitochondrial Metabolism
Caspase
|
Cancer
|
|
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects .
|
-
- HY-116926
-
|
|
Antibiotic
Bacterial
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Infection
Cancer
|
|
Deoxynybomycin is an antibiotic, that can be isolated from Streptomyces, and antibacterial activity against Staphylococcus aureus. Deoxynybomycin is the inhibitor for DNA gyrase and Topoisomerase I. Deoxynybomycin induces expression of p21/WAF1, exhibits cytotoxicity and induces apoptosis in cancer cells Saos-2, TMK-1, and THP-1 .
|
-
- HY-13768S2
-
|
SKF 104864A-d6 dihydrochloride; NSC 609669-d6 dihydrochloride
|
Isotope-Labeled Compounds
Apoptosis
Topoisomerase
Autophagy
|
Cancer
|
|
Topotecan-d6 dihydrochloride (SKF 104864A-d6 dihydrochloride) is the deuterium labeled Topotecan dihydrochloride. 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-13704R
-
|
7-Ethyl-10-hydroxycamptothecin (Standard)
|
Drug Metabolite
Reference Standards
Topoisomerase
ADC Payload
Autophagy
|
Cancer
|
|
SN-38 (Standard) is the analytical standard of SN-38. This product is intended for research and analytical applications. 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. SN-38 is a payload of sacituzumab govitecan (HY -132254) .
|
-
- HY-100620R
-
|
APC (Standard)
|
Drug Metabolite
Reference Standards
Topoisomerase
Cholinesterase (ChE)
|
Cancer
|
|
RPR121056 (Standard) is the analytical standard of RPR121056. This product is intended for research and analytical applications. 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[1].
|
-
- HY-P99843
-
|
|
TROP2
ADC Antibody
|
Cancer
|
|
Datopotamab (CDP7657) is a humanized anti trophoblast cell surface antigen 2 (TROP2) antibody. Datopotamab can generate antibody drug conjugates (ADC) (HY-141598) with DNA topoisomerase I inhibitor Deruxtecan (HY-13631E). Datopotamab can be used in the study of triple negative breast cancer and non-small cell lung cancer .
|
-
- HY-W653919
-
|
|
Isotope-Labeled Compounds
Drug Metabolite
|
Cancer
|
|
SN-38 glucuronide-d3 is deuterium labeled SN-38 glucuronide. SN-38 glucuronide is an inactive metabolite of the anticancer active molecule Irinotecan (HY-16562) and has toxic effects on the gastrointestinal tract. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
|
-
- HY-183912
-
|
|
Topoisomerase
ADC Payload
|
Cancer
|
|
PY-4Car2 is a Camptothecin (HY-16560) derivative and a topoisomerase I inhibitor. PY-4Car2 functions as a warhead conjugated via a cleavable linker to the bispecific ADC TJ101. PY-4Car2 can be used as an ADC payload for the research of cancers .
|
-
- HY-148696A
-
|
|
ADC Payload
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-175700
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
YCJ-02 is a selective Topoisomerase I (Top I) inhibitor. YCJ-02 can inhibit cell proliferation and induce apoptosis and G2/M phase arrest. YCJ-02 can induce DNA damage and increaseγ-H2AX levels. YCJ-02 can promote Top I deqradation via a ubiquitin/26S proteasome pathway. YCJ-02 increases the expressions of pro-apoptotic proteins Bad, Bax, and cleaved
caspase-3. YCJ-02 shows broad-spectrum antitumor activity. YCJ-02 can be used for the research of cancer, such as intrahepatic cholangiocarcinoma (ICC) .
|
-
- HY-W744739
-
-
- HY-175269
-
|
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Topoisomerase
|
Cancer
|
|
MGB1Y is a noncovalent DNA minor groove binder (MGB). MGB1Y potently inhibits cancer cells proliferation and topoisomerase I activity. MGB1Y downregulates their breast cancer-related genes in MCF7 and MDA-MB-231 cells. MGB1Y has a broad-spectrum anticancer activity, such as breast cancer, colon cancer, and leukemia .
|
-
- HY-N2108
-
|
|
Drug Derivative
Drug Intermediate
Topoisomerase
|
Cancer
|
|
7-Ethylcamptothecin is a derivative of Camptothecin (HY-16560) and a DNA topoisomerase I inhibitor that exhibits significant antitumor activity against tumor cells. 7-Ethylcamptothecin serves as a key precursor for the synthesis of 20 (S)-O-substituted benzoyl-7-ethylcamptothecin compounds. 7-Ethylcamptothecin is widely used in various tumor-related scientific studies .
|
-
- HY-141436R
-
|
Sucrose octasulfate potassium (Standard)
|
Biochemical Assay Reagents
Reference Standards
|
Cancer
|
|
Sucrosofate (potassium) (Standard) is the analytical standard of Sucrosofate (potassium). This product is intended for research and analytical applications. Sucrosofate (Sucrose octasulfate) potassium is a sucrose acid that can be used to prepare liposomes to deliver Irinotecan (HY-16562). Irinotecan is an inhibitor of topoisomerase Topo I and is commonly used in colon and rectal cancer research. Sucrosofate nanoliposome preparation loaded with Irinotecan, also known as PEP02 or MM-398 .
|
-
- HY-131438
-
|
|
Topoisomerase
|
Cancer
|
|
GI-149893 is a selective topoisomerase I (TopoI) inhibitor. GI-149893 prevents DNA religation and induces irreversible DNA damage in tumor cells. GI-149893 is promising for research of cancers (e.g., colon carcinoma HT-29/SW-48, breast MX-1, prostate PC-3 xenografts) .
|
-
- HY-179520
-
|
|
Topoisomerase
DNA/RNA Synthesis
MDM-2/p53
Bcl-2 Family
|
Cancer
|
|
XSJ151 is a topoisomerase I inhibitor, stabilizing the DNA-Topo I covalent complex and inducing DNA double-strand breaks. XSJ151-induces DNA damage activates the p53-p21 signaling pathway, specifically regulating the expression of cyclins, leading to G2/M phase cell cycle arrest and disrupting the dynamic homeostasis of Bcl-2 family proteins, thereby triggering apoptosis in gastric cancer cells. XSJ151 can be used for the study of gastric cancer .
|
-
- 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-164152
-
|
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
|
ADC Control Human IgG1-Deruxtecan (DAR 4) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
|
-
- HY-164152A
-
|
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
|
ADC Control Human IgG1-Deruxtecan (DAR 8) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
|
-
- HY-156376
-
|
|
Cuproptosis
Apoptosis
Topoisomerase
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
Cancer
|
|
Cu(II)-Elesclomol is a complex formed by Elesclomol (HY-12040) and Cu 2+ (copper ions). Cu(II)-Elesclomol is also a weak inhibitor of DNA topoisomerase I. Cu(II)-Elesclomol exerts anticancer effects by inducing oxidative stress and DNA damage through copper chelation. Cu(II)-Elesclomol can inhibit tumor cell proliferation and induce cell cycle arrest and apoptosis. Cu(II)-Elesclomol can be used in the study of cancer .
|
-
- HY-101647R
-
|
RP 60475 (Standard)
|
Topoisomerase
Reference Standards
|
Cancer
|
|
Intoplicine (Standard) is the analytical standard of Intoplicine (HY-101647). This product is intended for research and analytical applications. 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 105 /M) and thereby increases the length of linear DNA .
|
-
- HY-126373S
-
|
SN-38G-d5
|
Isotope-Labeled Compounds
Drug Metabolite
|
Cancer
|
|
SN-38 glucuronide-d5 (SN-38G-d5) is the deuterium labeled SN-38 glucuronide (HY-126373). SN-38 glucuronide is an inactive metabolite of the anticancer active molecule Irinotecan (HY-16562) and has toxic effects on the gastrointestinal tract. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer.
|
-
- 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 .
|
-
- HY-153067
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan (Compound 11) is a bioactive compound-linker conjugate for ADC. Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan can conjugate with antibodies to form ADC (C-11) with anti-tumor activity. Exatecan is a DNA Topoisomerase I inhibitor. Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan can be used in the research of squamous cell carcinoma, pancreatic adenocarcinoma and colorectal cancer .
|
-
- HY-162472
-
|
|
ATM/ATR
DNA-PK
|
Cancer
|
|
XRD-0394 is a potent and orally active dual ATM and DNA-PKcs inhibitor with IC50s of 0.39 nM and 0.89 nM, respectively. XRD-0394 shows selectivity over other PIKK and PI3K family members. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro .
|
-
- HY-156513
-
|
7-Hydroxyethyl carbamate-(10Me-11F-Camptothecin)
|
ADC Payload
|
Cancer
|
|
ZD06519 (7-Hydroxyethyl carbamate-(10Me-11F-Camptothecin)) is a camptothecin (HY-16560) analogue and a topoisomerase I inhibitor. ZD06519 is an ADC cytotoxin with a strong bystander effect, inhibiting a variety of malignancies such as HER2-positive and FRα-overexpressing tumors. ZD06519 inhibits DNA cleavage, relaxation, and reconnection processes, inducing tumor cell death. ZD06519 can be used for ADC synthesis and cancer research .
|
-
- 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.
|
-
- HY-164762
-
|
SHR-A1811
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
|
Trastuzumab rezetecan (SHR-A1811) is a HER2-targeting antibody-drug conjugate (ADC). Trastuzumab rezetecan is composed of a humanized anti-HER2 antibody (HY-P9907), a cleavable linker MC-Gly-Gly-Phe-Gly (HY-44246), and a topoisomerase I inhibitor payload Rezetecán (HY-147408). Trastuzumab rezetecan can be used for research in HER2-positive breast cancer .
|
-
- HY-160005
-
|
NSC 781517
|
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
LMP517 (NSC 781517) is a potent and non-camptothecin Topoisomerase I and II (TOP1 and TOP2) dual inhibitor. LMP517 can induce TOP1 and TOP2 cleavage complexes (TOP1ccs and TOP2ccs). LMP517 can induce cancer cells DNA damage and γH2AX production. LMP517 can be used for the research of cancer, such as small cell lung cancer .
|
-
- HY-161501
-
|
|
GLUT
Topoisomerase
Apoptosis
|
Cancer
|
|
3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity .
|
-
- HY-13768S
-
|
SKF 104864A-d5; NSC 609669-d5
|
Isotope-Labeled Compounds
Topoisomerase
Autophagy
|
Cancer
|
|
Topotecan-d5 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±0.24 μM of GSCs-U87 .
|
-
- HY-W046353R
-
|
o-Methoxycinnamaldehyde (Standard)
|
Reference Standards
Apoptosis
NF-κB
Mitochondrial Metabolism
Caspase
Topoisomerase
|
Cancer
|
|
2-Methoxycinnamaldehyde (Standard) is the analytical standard of 2-Methoxycinnamaldehyde. This product is intended for research and analytical applications. 2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects .
|
-
- HY-101647AR
-
|
RP 60475 dimesylate (Standard)
|
Topoisomerase
Reference Standards
|
Cancer
|
|
Intoplicine (dimesylate) (Standard) is the analytical standard of Intoplicine (dimesylate) (HY-101647A). This product is intended for research and analytical applications. 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 105 /M) and thereby increases the length of linear DNA .
|
-
- 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-185683
-
|
DB-1311; BNT324
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
CD276/B7-H3
|
Cancer
|
|
Elfetabart drozuntecan (DB-1311; BNT324) is an antibody-drug conjugate (ADC) targeting B7H3. Elfetabart drozuntecan conjugates a humanized anti-B7H3 IgG1 monoclonal antibody with a topoisomerase I inhibitor via a cleavable linker. Elfetabart drozuntecan exerts antitumor activity in solid tumors. Elfetabart drozuntecan can be used for the research of advanced/metastatic solid tumors .
|
-
- HY-173625
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
P5(PEG12)-VC-PAB-Exatecan (LP3) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG12)-VC-PAB-Exatecan can be used for the research of tumor .
|
-
- HY-155073
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
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) .
|
-
- HY-16055
-
|
AR-67; DB 67
|
Topoisomerase
Drug Derivative
MDM-2/p53
|
Cancer
|
|
Silatecan (AR-67) is a blood-brain barrier-permeable derivative of Camptothecin (HY-16560), DNA topoisomerase I inhibitor, an anticancer agent, and a radiosensitizer. Silatecan potently radiosensitizes wild-type p53 gliomas. Silatecan can be used in research related to glioma, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer, breast cancer, cervical cancer, gastric cancer, nasopharyngeal cancer, and uterine cancer .
|
-
- HY-N0095S
-
|
10-HCPT-d5; 10-Hydroxycamptothecin-d5
|
Isotope-Labeled Compounds
Apoptosis
Topoisomerase
|
Cancer
|
|
(S)-10-Hydroxycamptothecin-d5 (10-HCPT-d5) is the deuterium labeled (S)-10-Hydroxycamptothecin. (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia research .
|
-
- HY-171747
-
|
|
Antibody-Drug Conjugates (ADCs)
EGFR
Topoisomerase
Apoptosis
|
Cancer
|
|
AMT-562 is an antibody-drug conjugate (ADC) consisting of a novel anti-HER3 antibody Ab562 (HY-P991505) conjugated to the linker MC-VA-PAB and the topoisomerase I inhibitor Exatecan (HY-13631). The ADC toxic molecule and linker portion are MC-VA-PAB-Exatecan (HY-147270). AMT-562 can induce apoptosis and has antitumor activity against pancreatic, esophageal, and gastric cancers .
|
-
- HY-118899
-
|
|
Endogenous Metabolite
|
Cancer
|
|
XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
|
-
- HY-B0147A
-
|
Pefloxacinium mesylate
|
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin (Pefloxacinium) mesylate is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin mesylate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate can be used for infection studies .
|
-
- HY-13704S2
-
|
7-Ethyl-10-hydroxycamptothecin-13C6
|
Isotope-Labeled Compounds
Autophagy
ADC Payload
Topoisomerase
Drug Metabolite
|
Infection
Cancer
|
|
SN-38- 13C6 (7-Ethyl-10-hydroxycamptothecin- 13C6) is the 13C-labeled SN-38 (HY-13704). SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 can bind to RPL15. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254) .
|
-
- HY-B0147
-
|
Pefloxacinium
|
Antibiotic
Bacterial
Parasite
DNA/RNA Synthesis
Topoisomerase
|
Infection
Inflammation/Immunology
|
|
Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
- HY-162805
-
|
|
NO Synthase
Topoisomerase
Apoptosis
NF-κB
|
Inflammation/Immunology
Cancer
|
|
iNOS/TopoI-IN-1 (compound AuL9) is a multi-target hybrid molecule with anti-tumor, anti-inflammatory and antioxidant activities. iNOS/TopoI-IN-1 inhibits the growth of breast cancer cells MCF-7 and MDA MB-231 in vitro with IC50 of 3.5 μM and 6.3 μM, respectively, and induces DNA damage and apoptosis of breast cancer cells by inhibiting human topoisomerase I (TopoI) (Ki=2.72 μM). In addition, NOS/TopoI-IN-1 inhibits the expression of iNOS by inhibiting the activation of NF-kB (Ki=1.49 μM) .
|
-
- HY-171124
-
|
AZD9592
|
Antibody-Drug Conjugates (ADCs)
EGFR
c-Met/HGFR
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
Tilatamig samrotecan (AZD9592) is an anti-EGFR/c-MET antibody-drug conjugate (ADC). Tilatamig samrotecan consists of an anti-EGFR/c-MET antibody with the drug-linker conjugate being AZ14170133 (HY-145399) (a topoisomerase I (TOP1i) inhibitor payload). Tilatamig samrotecan induces multiple DNA damage response pathway markers (like ATM, ATR, γH2AX). Tilatamig samrotecan selectively binds to EGFR and c-MET, delivering the cytotoxic payload. Tilatamig samrotecan exerts anti-tumor activity in vivo. Tilatamig samrotecan can be used for non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) research .
|
-
- HY-138298
-
|
T-DXd (solution); DS-8201 (solution); DS-8201a (solution)
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
|
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), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .
|
-
- HY-128946
-
|
|
Drug-Linker Conjugates for ADC
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- HY-138298A
-
|
T-DXd; 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), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .
|
-
- HY-177681
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(Mal)-N-(PEG8-Val-Cit-PAB-MMAE)-N-(PEG8-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Mal)-N-(PEG8-Val-Cit-PAB-MMAE)-N-(PEG8-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-173703
-
|
|
Topoisomerase
Drug Intermediate
|
Cancer
|
|
β-Glu-PAB(CH2NH2)-Exatecan (Compound 9a) is a topoisomerase I inhibitor. β-Glu-PAB(CH2NH2)-Exatecan binds to the topoisomerase I-DNA complex to prevent DNA strand reconnection, thereby inducing DNA breakage and cell apoptosis. β-Glu-PAB(CH2NH2)-Exatecan can be specifically cleaved by β-glucuronidase highly expressed in the tumor microenvironment to release Exatecan for cytotoxic effect. β-Glu-PAB(CH2NH2)-Exatecan is also an intermediate of Mal((3S,3aR,6S,6aR) -hexahydrofuro [3, 2-B]furan-3,6-diamine-PEG12)-β -Glu-Pab-Exatecan. β-Glu-PAB(CH2NH2)-Exatecan is promising for research of cancers .
|
-
- HY-185101
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
MC-AcLys-GDEVD-PABC-Exatecan (MC-AcLys-GDEVD-PABC-DX8951) is a agent-linker conjugate for ADC. MC-AcLys-GDEVD-PABC-Exatecan is a DX8951 (a DNA topoisomerase I inhibitor) derivative with a novel caspase-3 cleavable peptide linker MC-AcLys-GDEVD-PABC linker. MC-AcLys-GDEVD-PABC-Exatecan can be used to prepare DX8951 antibody conjugate (ADC), and it exhibites significant bystander effect mediated by the caspase-3-triggered extracellular cleavage of the linker, enhancing payload release into the tumor microenvironment.
|
-
- HY-N0095R
-
|
10-HCPT (Standard); 10-Hydroxycamptothecin (Standard)
|
Reference Standards
Topoisomerase
Apoptosis
|
Cancer
|
|
(S)-10-Hydroxycamptothecin (Standard) is the analytical standard of (S)-10-Hydroxycamptothecin. This product is intended for research and analytical applications. (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-B0147B
-
|
Pefloxacinium mesylate dihydrate
|
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin (Pefloxacinium) mesylate dihydrate is a broad spectrum antibiotic. Pefloxacin mesylate dihydrate blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate dihydrate inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin mesylate dihydrate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate dihydrate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate dihydrate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate dihydrate can be used for infection studies .
|
-
- HY-178738
-
|
|
Antibiotic
Bacterial
Topoisomerase
DNA/RNA Synthesis
|
Infection
|
|
GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis .
|
-
- HY-13631J
-
|
(1R,9R)-DX8951f
|
Drug Derivative
Topoisomerase
Apoptosis
|
Cancer
|
(1R,9R)-Exatecan mesylate ((1R,9R)-DX8951f) is a non-prodrug camptothecin derivative and a potent topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan mesylate is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia . The low-activity isomer of (1R,9R)-Exatecan mesylate is (1S,9R)-Exatecan mesylate (HY-13631I).
|
-
- HY-P992103
-
|
BNT326/YL202 Antibody
|
ADC Payload
|
Cancer
|
|
Beruzatatug (BNT326/YL202 Antibody) is an IgG1 monoclonal antibody against HER3. Beruzatatug can be used for the synthesis of ADCs, such as BNT326/YL202 .
|
-
- HY-171684
-
|
|
Antibody-Drug Conjugates (ADCs)
CCR
Topoisomerase
|
Cancer
|
|
Anti-CCL2 (Carlumab)-MC-Vc-PAB-SN38 is an antibody-drug conjugate (ADC) consisting of the humanized anti-CCL2 (chemokine ligand 2) antibody Carlumab (HY-P99188) conjugated to the linker Mc-VC-PAB and the topoisomerase I inhibitor SN38 (HY-13704). The ADC toxic molecule and linker part are Mc-VC-PAB-SN38 (HY-131057). Anti-CCL2 (Carlumab)-MC-Vc-PAB-SN38 can be used in cancer research .
|
-
- HY-177683
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(DBCO-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(DBCO-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177678
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177686
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177685
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(TCO-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(TCO-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177679
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(Amino-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Amino-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177687
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(Mal-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Mal-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177682
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177684
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(endo-BCN-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(endo-BCN-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177688
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177680
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Others
|
|
N-(Mal-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Mal-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-178145
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan (compound 12) is a Drug-Linker Conjugate for ADC. Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan contains the ADC linker (Mc-Lys(PEG12)-Cap-Ala-Ala-PABC) (HY-178146) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan can be used for the development of ADC targeting HER2-positive breast cancer .
|
-
- HY-B0147R
-
|
Pefloxacinium (Standard)
|
Reference Standards
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin (Standard) (Pefloxacinium (Standard)) is the analytical standard of Pefloxacin (HY-B0147). This product is intended for research and analytical applications. Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
- HY-B0147AR
-
|
Pefloxacinium mesylate (Standard)
|
Reference Standards
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin mesylate (Standard) (Pefloxacinium mesylate (Standard)) is the analytical standard of Pefloxacin mesylate (HY-B0147A). This product is intended for research and analytical applications. Pefloxacin (Pefloxacinium) mesylate is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin mesylate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate can be used for infection studies .
|
-
- HY-B0147S1
-
|
Pefloxacinium-d3
|
Isotope-Labeled Compounds
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin-d3 (Pefloxacinium-d3) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
- HY-B0147S
-
|
Pefloxacinium-d5
|
Isotope-Labeled Compounds
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin-d5 (Pefloxacinium-d5) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
- HY-B0147BR
-
|
Pefloxacinium mesylate dihydrate (Standard)
|
Reference Standards
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin (Pefloxacinium) mesylate dihydrate (Standard) is the analytical standard of Pefloxacin mesylate dihydrate (HY-B0147B). This product is intended for research and analytical applications. Pefloxacin (Pefloxacinium) mesylate dihydrate is a broad spectrum antibiotic. Pefloxacin mesylate dihydrate blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate dihydrate inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin mesylate dihydrate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate dihydrate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate dihydrate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate dihydrate can be used for infection studies .
|
-
- HY-171738
-
|
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
Sodium Channel
|
Cancer
|
|
Anti-SLC34A2 (Lifastuzumab)-MC-Vc-PAB-SN38 is an antibody-drug conjugate (ADC) consisting of the humanized anti-SLC34A2 (sodium-dependent phosphate transporter 2) antibody Lifastuzumab (HY-P99970) conjugated to the linker Mc-VC-PAB and the topoisomerase I inhibitor SN38 (HY-13704). The ADC toxic molecule and linker part are Mc-VC-PAB-SN38 (HY-131057). Anti-SLC34A2 (Lifastuzumab)-MC-Vc-PAB-SN38 can be used in cancer research .
|
-
- HY-P3371
-
|
DS-7300a; MABX-9001a; I-DXd
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
Apoptosis
|
Cancer
|
|
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
|
-
- HY-183594
-
|
|
Drug-Linker Conjugates for ADC
|
Others
|
|
Exatecan-(D-2,4-DHB)-NH2-AA (bPEG8)-Mal is a linker-payload conjugate. Exatecan-(D-2,4-DHB)-NH2-AA (bPEG8)-Mal contains the linker D-2,4-DHB-NH2-AA(bPEG8)-Mal (HY-183595) and the cytotoxic agent Exatecan (HY-13631), a potent DNA topoisomerase I inhibitor. Exatecan-(D-2,4-DHB)-NH2-AA (bPEG8)-Mal can be utilized for the development of antibody-drug conjugates (ADCs) .
|
-
- HY-141598
-
|
DS-1062 (solution); Dato-DXd (solution)
|
TROP2
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
|
Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer .
|
-
- HY-P990059
-
|
INT-016; AZD8205 Antibody
|
ADC Antibody
CD276/B7-H3
|
Cancer
|
|
Puxitatug (INT-016; AZD8205 Antibody) is a monoclonal antibody targeting VTCN1/B7-H4. Puxitatug can be used to synthesize antibody-drug conjugates (ADCs), such as Puxitatug samrotecan (HY-171689), which can be applied to various solid tumors. Puxitatug can also be used for researching adjuvant therapies for gastric cancer .
|
-
- HY-173634
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan (LP1) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB (HY-173635) to make antibody agent conjugate (ADC), AZD0516 (HY-173639) .
|
-
![Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan](//file.medchemexpress.com/product_pic/hy-173634.gif)
- HY-13631I
-
|
(1S,9R)-DX8951f
|
Drug Derivative
Topoisomerase
Apoptosis
|
Cancer
|
(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is a non-prodrug camptothecin derivative and a topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1S,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1S,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1S,9R)-Exatecan mesylate is widely used in preclinical studies of various cancers such as pancreatic cancer, lung cancer, breast cancer, and leukemia .
The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).
|
-
- HY-Y0790R
-
|
p-Isopropylbenzaldehyde (Standard)
|
α-synuclein
Reference Standards
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Cuminaldehyde Standard is the analytical standard of Cuminaldehyde. This product is intended for research and analytical applications. Cuminaldehyde is the main component of Cuminum cyminum and has multiple biological activities, including anti-inflammatory, anti-cancer, anti-diabetic, anti-injury, anti-neuropathy and antibacterial effects. Cuminaldehyde is an inhibitor of aldose reductase (IC50= 0.00085 mg/mL) and α-glucosidase (IC50=0.5 mg/mL). Cuminaldehyde also inhibits the fibrillation of α-synuclein and prevents its aggregation Cuminaldehyde can induce apoptosis in colon adenocarcinoma cells by targeting topoisomerase I and II. In addition, Cuminaldehyde also exerts anti-inflammatory activity by inhibiting lipoxygenase. Cuminaldehyde has a strong inhibitory effect on the growth of Aspergillus flavus and the biosynthesis of aflatoxin B1 (AFB1). Cuminaldehyde can exert anti-injury and anti-neuropathy effects by participating in opioid receptors, L-arginine/NO/cGMP pathways and anti-inflammatory effects. Cuminaldehyde has potential application value in the research of neurodegenerative diseases, cancer, diabetes and neuropathic pain diseases .
|
-
- HY-P992026
-
|
|
ADC Antibody
|
Cancer
|
|
ADV-101 Antibody is a monoclonal antibody inhibitor targeting IL-1RAP. ADV-101 Antibody can be used to synthesize the antibody-drug conjugate (ADC) ADV-101. ADV-101 Antibody can be used to research related to cancer .
|
-
- HY-177442
-
|
DS-3939
|
Antibody-Drug Conjugates (ADCs)
Mucin
Topoisomerase
Apoptosis
|
Cancer
|
|
DS-3939a (DS-3939) is an anti-TA-MUC1 (tumor-associated mucin-1) antibody-drug conjugate (ADC). DS-3939a consists of a humanized anti-TA-MUC1 IgG1 monoclonal antibody Gatipotuzumab ( HY-P99634), a stable and cleavable tetrapeptide-based linker (Gly-Gly-Phe-Gly), and a DNA topoisomerase I inhibitor payload (DXd) (HY-13631D), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). DS-3939a inhibits the growth of TA-MUC1-positive cancer cells (CFPAC-1, NCI-H2110) by inducing DNA damage and apoptosis. DS-3939a exhibits significant antitumor activity in a variety of TA-MUC1-expressing advanced solid tumors. DS-3939a can be used for the study of TA-MUC1-expressing advanced cancers .
|
-
- HY-182759
-
|
|
DNA Alkylator/Crosslinker
Topoisomerase
Caspase
Bcl-2 Family
Apoptosis
|
Cancer
|
|
MN33-47 is a multi-target anti-tumor compound with broad-spectrum anti-proliferative activity. MN33-47 relieves the inhibition of the mitochondrial apoptosis pathway by downregulating the anti-apoptotic protein Bcl-2, while activating caspase-3 and inhibiting Topoisomerase I activity, thereby promoting its degradation through the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-47 can also induce DNA cross-linking and G2/M cell cycle arrest, inhibit cancer cell migration and activate the mitochondrial apoptosis pathway, thus exerting potent anti-tumor effects. MN33-47 can improve the water solubility of SN-38 (HY-13704), and exhibits dose-dependent tumor growth inhibition effects in CT26 tumor-bearing mouse models without obvious toxic and side effects. MN33-47 can be used in related studies on colorectal adenocarcinoma, cervical adenocarcinoma, hepatocellular carcinoma, alveolar basal epithelial adenocarcinoma, gastric cancer and colon cancer .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-138298
-
|
T-DXd (solution); DS-8201 (solution); DS-8201a (solution)
|
Fluorescent Dyes
|
|
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), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .
|
-
- HY-138298A
-
|
T-DXd; DS-8201; DS-8201a
|
Fluorescent Dyes
|
|
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), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .
|
-
- HY-141598
-
|
DS-1062 (solution); Dato-DXd (solution)
|
Fluorescent Dyes
|
|
Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer .
|
-
- HY-164789
-
|
SKB264; MK-2870
|
Fluorescent Dyes
|
|
Sacituzumab tirumotecan is an antibody-drug conjugate and TROP2-directed, topoisomerase I inhibitor payload-delivering agent, with a TROP2 EC50 of 2.787 ng/ml, TROP2 Ka of 0.3083 nM, and topoisomerase I IC50 of 0.7 μmol/L. Sacituzumab tirumotecan can be used for the research of metastatic triple-negative breast cancer, and metastatic non-small cell lung cancer .
|
-
- HY-P3371
-
|
DS-7300a; MABX-9001a; I-DXd
|
Fluorescent Dyes
|
|
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
|
-
- HY-164152A
-
|
|
Fluorescent Dyes
|
|
ADC Control Human IgG1-Deruxtecan (DAR 8) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
|
-
- HY-164152
-
|
|
Fluorescent Dyes
|
|
ADC Control Human IgG1-Deruxtecan (DAR 4) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
|
-
- HY-13631AG
-
|
DX8951f
|
Fluorescent Dyes
|
|
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 .
|
-
- HY-177442
-
|
DS-3939
|
Fluorescent Dyes
|
|
DS-3939a (DS-3939) is an anti-TA-MUC1 (tumor-associated mucin-1) antibody-drug conjugate (ADC). DS-3939a consists of a humanized anti-TA-MUC1 IgG1 monoclonal antibody Gatipotuzumab ( HY-P99634), a stable and cleavable tetrapeptide-based linker (Gly-Gly-Phe-Gly), and a DNA topoisomerase I inhibitor payload (DXd) (HY-13631D), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). DS-3939a inhibits the growth of TA-MUC1-positive cancer cells (CFPAC-1, NCI-H2110) by inducing DNA damage and apoptosis. DS-3939a exhibits significant antitumor activity in a variety of TA-MUC1-expressing advanced solid tumors. DS-3939a can be used for the study of TA-MUC1-expressing advanced cancers .
|
-
- HY-164762
-
|
SHR-A1811
|
Fluorescent Dyes
|
|
Trastuzumab rezetecan (SHR-A1811) is a HER2-targeting antibody-drug conjugate (ADC). Trastuzumab rezetecan is composed of a humanized anti-HER2 antibody (HY-P9907), a cleavable linker MC-Gly-Gly-Phe-Gly (HY-44246), and a topoisomerase I inhibitor payload Rezetecán (HY-147408). Trastuzumab rezetecan can be used for research in HER2-positive breast cancer .
|
-
- HY-N2306R
-
|
Aclarubicin (Standard)
|
Fluorescent Dyes
|
|
Aclacinomycin A (Standard) is the analytical standard of Aclacinomycin A. This product is intended for research and analytical applications. 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-171747
-
|
|
Fluorescent Dyes
|
|
AMT-562 is an antibody-drug conjugate (ADC) consisting of a novel anti-HER3 antibody Ab562 (HY-P991505) conjugated to the linker MC-VA-PAB and the topoisomerase I inhibitor Exatecan (HY-13631). The ADC toxic molecule and linker portion are MC-VA-PAB-Exatecan (HY-147270). AMT-562 can induce apoptosis and has antitumor activity against pancreatic, esophageal, and gastric cancers .
|
| Cat. No. |
Product Name |
Type |
-
- HY-13631AG
-
|
DX8951f
|
Biochemical Assay Reagents
|
|
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 .
|
-
- HY-143692
-
|
|
Biochemical Assay Reagents
|
|
SQDG inhibits topoisomerase I and P-selectin receptor, exhibits anti-inflammatory, antiviral and antitumor activities. SQDG is a glycolipid that possesses sugar moieties in their head groups. SQDG is a membrane lipid that can be used to investigate the effects of structural lipid in LNP formulations .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10765
-
|
|
Peptide-Drug Conjugates (PDCs)
Topoisomerase
|
Cancer
|
|
DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99843
-
|
|
TROP2
ADC Antibody
|
Cancer
|
|
Datopotamab (CDP7657) is a humanized anti trophoblast cell surface antigen 2 (TROP2) antibody. Datopotamab can generate antibody drug conjugates (ADC) (HY-141598) with DNA topoisomerase I inhibitor Deruxtecan (HY-13631E). Datopotamab can be used in the study of triple negative breast cancer and non-small cell lung cancer .
|
-
(5)
-
- HY-P3371
-
|
DS-7300a; MABX-9001a; I-DXd
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
Apoptosis
|
Cancer
|
|
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
|
-
(5)
-
- HY-164152
-
|
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
|
ADC Control Human IgG1-Deruxtecan (DAR 4) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
|
-
(5)
-
- HY-P990059
-
|
INT-016; AZD8205 Antibody
|
ADC Antibody
CD276/B7-H3
|
Cancer
|
|
Puxitatug (INT-016; AZD8205 Antibody) is a monoclonal antibody targeting VTCN1/B7-H4. Puxitatug can be used to synthesize antibody-drug conjugates (ADCs), such as Puxitatug samrotecan (HY-171689), which can be applied to various solid tumors. Puxitatug can also be used for researching adjuvant therapies for gastric cancer .
|
-
(5)
-
- HY-P992124
-
|
BAT8006 Antibody; BAT-6028
|
Folate Receptor (FR)
|
Cancer
|
|
Onvontatug (BAT8006 Antibody) is a humanized monoclonal antibody targeting folate receptor α (FRα). Onvontatug can be used to construct antibody-drug conjugates (ADCs), such as BAT8006. It is applicable to research related to platinum-resistant ovarian cancer .
|
-
(5)
-
- HY-P992130
-
|
TQB2102 Antibody
|
ADC Antibody
EGFR
|
Cancer
|
|
Rolditamig (TQB2102 Antibody) is a recombinant humanized anti-human epidermal growth factor receptor 2 (HER2) antibody. Rolditamig can be conjugated with an enzyme-cleavable linker and a topoisomerase I inhibitor to form the ADC TQB2102. Rolditamig is applicable to research on solid tumors such as HER2-positive breast cancer .
|
-
(5)
-
- HY-P992103
-
|
BNT326/YL202 Antibody
|
ADC Payload
|
Cancer
|
|
Beruzatatug (BNT326/YL202 Antibody) is an IgG1 monoclonal antibody against HER3. Beruzatatug can be used for the synthesis of ADCs, such as BNT326/YL202 .
|
-
(5)
-
- HY-P992026
-
|
|
ADC Antibody
|
Cancer
|
|
ADV-101 Antibody is a monoclonal antibody inhibitor targeting IL-1RAP. ADV-101 Antibody can be used to synthesize the antibody-drug conjugate (ADC) ADV-101. ADV-101 Antibody can be used to research related to cancer .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-15142
-
-
-
- HY-13704
-
-
-
- HY-16560
-
-
-
- HY-13768A
-
-
-
- HY-16562A
-
-
-
- HY-10529
-
-
-
- HY-A0210
-
-
-
- HY-N2306
-
-
-
- HY-15142R
-
-
-
- HY-13555
-
-
-
- HY-15142A
-
-
-
- HY-N6800A
-
-
-
- HY-N0095
-
-
-
- HY-B0147
-
|
Pefloxacinium
|
Infection
Classification of Application Fields
Disease Research Fields
|
Antibiotic
Bacterial
Parasite
DNA/RNA Synthesis
Topoisomerase
|
|
Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
-
- HY-13744
-
-
-
- HY-N2108
-
-
-
- HY-N3488
-
-
-
- HY-100309
-
-
-
- HY-N6714
-
-
-
- HY-N5038
-
-
-
- HY-W046353
-
-
-
- HY-13704R
-
-
-
- HY-N0275
-
-
-
- HY-N2306A
-
-
-
- HY-N10495
-
-
-
- HY-10529R
-
-
-
- HY-N2306R
-
-
-
- HY-19825
-
-
-
- HY-N6800
-
-
-
- HY-W713570
-
-
-
- HY-16560R
-
-
-
- HY-Y0790R
-
|
p-Isopropylbenzaldehyde (Standard)
|
Structural Classification
Ketones, Aldehydes, Acids
Rudbeckia laciniata L.
Umbelliferae
Plants
Endogenous metabolite
Source Classification
|
α-synuclein
Reference Standards
|
|
Cuminaldehyde Standard is the analytical standard of Cuminaldehyde. This product is intended for research and analytical applications. Cuminaldehyde is the main component of Cuminum cyminum and has multiple biological activities, including anti-inflammatory, anti-cancer, anti-diabetic, anti-injury, anti-neuropathy and antibacterial effects. Cuminaldehyde is an inhibitor of aldose reductase (IC50= 0.00085 mg/mL) and α-glucosidase (IC50=0.5 mg/mL). Cuminaldehyde also inhibits the fibrillation of α-synuclein and prevents its aggregation Cuminaldehyde can induce apoptosis in colon adenocarcinoma cells by targeting topoisomerase I and II. In addition, Cuminaldehyde also exerts anti-inflammatory activity by inhibiting lipoxygenase. Cuminaldehyde has a strong inhibitory effect on the growth of Aspergillus flavus and the biosynthesis of aflatoxin B1 (AFB1). Cuminaldehyde can exert anti-injury and anti-neuropathy effects by participating in opioid receptors, L-arginine/NO/cGMP pathways and anti-inflammatory effects. Cuminaldehyde has potential application value in the research of neurodegenerative diseases, cancer, diabetes and neuropathic pain diseases .
|
-
-
- HY-N15319
-
|
Canangine
|
Alkaloids
Other Alkaloids
Cananga odorata
Plants
Annonaceae
Source Classification
|
Topoisomerase
Fungal
|
|
Eupolauridine (Canangine) is a selective DNA topoisomerase II inhibitor with IC50 values of 20 μM for fungal topoisomerase I and 33 μM for human topoisomerase I. Eupolauridine exerts antifungal activity by inhibiting the catalytic activity of topoisomerase II and stabilizing its cleavage complex with DNA, leading to DNA damage. Eupolauridine is promising for research of fungal infectious diseases .
|
-
-
- HY-N10115
-
-
-
- HY-W897655
-
-
-
- HY-N10367
-
-
-
- HY-13768AR
-
-
-
- HY-N6714R
-
-
-
- HY-16562AR
-
-
-
- HY-N0275R
-
-
-
- HY-N11536
-
-
-
- HY-13555R
-
-
-
- HY-W046353R
-
-
-
- HY-N0095R
-
-
-
- HY-N4329
-
-
-
- HY-N8250
-
-
-
- HY-N15249
-
|
Isovalerylspiramycin I; Shengjimycin E
|
Structural Classification
Natural Products
Microorganisms
Source Classification
|
Topoisomerase
DNA/RNA Synthesis
Checkpoint Kinase (Chk)
Apoptosis
Bacterial
|
|
4"-Isovalerylspiramycin I (Isovalerylspiramycin I) is a topoisomerase 1 (TOP1) inhibitor and an antitumor agent. 4"-Isovalerylspiramycin I directly binds to TOP1, suppresses DNA replication, and induces DNA damage. 4"-Isovalerylspiramycin I downregulates phosphorylated CHEK1 and the ATR/CHEK1 DNA damage repair pathway, blocks DNA repair, and augments DNA damage. 4"-Isovalerylspiramycin I suppresses proliferation, migration, and invasion of osteosarcoma cells. 4"-Isovalerylspiramycin I induces apoptosis and cell cycle arrest in osteosarcoma cells. 4"-Isovalerylspiramycin I exerts antibacterial activity against methicillin-resistant Staphylococcus aureus. 4"-Isovalerylspiramycin I can be used for the research of osteosarcoma, upper respiratory bacterial infections, and methicillin-resistant Staphylococcus aureus infection .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13631AS
-
|
|
|
Exatecan-d5 (DX8951f-d5) mesylate is deuterium labeled Exatecan mesylate (HY-13631A). Exatecan mesylate 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 .
|
-
-
- HY-13631DS
-
|
|
|
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) .
|
-
-
- HY-13704S
-
|
|
|
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 .
|
-
-
- HY-13566AS
-
|
|
|
Belotecan-d7 (hydrochloride) is the deuterium labeled Belotecan hydrochloride. Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative .
|
-
-
- HY-16562S1
-
|
|
|
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 .
|
-
-
- HY-126373S1
-
|
|
|
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-16560S
-
|
|
|
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 . 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-W744739
-
|
|
|
Betulinic acid-d3 (Lupatic acid-d3) is a deuterium labeled Betulinic acid (HY-10529). Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties . Betulinic acid can cross the blood-brain barrier.
|
-
-
- HY-13768S1
-
|
|
|
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 .
|
-
-
- HY-W653896
-
|
|
|
Alternariol-d2 is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
|
-
-
- HY-13631AS1
-
|
|
|
Exatecan-d3 (DX8951f-d3) mesylate is deuterium-labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL .
|
-
-
- HY-16562S
-
|
|
|
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 .
|
-
-
- HY-16562AS
-
|
|
|
Irinotecan-d5 hydrochloride is deuterated labeled Irinotecan hydrochloride (HY-16562A). Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer .
|
-
-
- HY-132561S
-
|
|
|
RPR121056-d3 is the deuterium labeled RPR121056. RPR121056 is a metabolite of Irinotecan (HY-16562), 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 study of colorectal cancer. Irinotecan also directly inhibits AChE .
|
-
-
- HY-W653919
-
|
|
|
SN-38 glucuronide-d3 is deuterium labeled SN-38 glucuronide. SN-38 glucuronide is an inactive metabolite of the anticancer active molecule Irinotecan (HY-16562) and has toxic effects on the gastrointestinal tract. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
|
-
-
- HY-13768S
-
|
|
|
Topotecan-d5 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±0.24 μM of GSCs-U87 .
|
-
-
- HY-N0095S
-
|
|
|
(S)-10-Hydroxycamptothecin-d5 (10-HCPT-d5) is the deuterium labeled (S)-10-Hydroxycamptothecin. (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia research .
|
-
-
- HY-B0147S1
-
|
|
|
Pefloxacin-d3 (Pefloxacinium-d3) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
-
- HY-B0147S
-
|
|
|
Pefloxacin-d5 (Pefloxacinium-d5) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
-
- HY-16562S2
-
|
|
|
Irinotecan- 13C6 ((+)-Irinotecan- 13C6) is the 13C-labeled Irinotecan (HY-16562). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
|
-
-
- HY-42487S1
-
|
|
|
Exatecan Intermediate 1-d2 is the deuterium labeled Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor with anticancer effects.
|
-
-
- HY-13768S2
-
|
|
|
Topotecan-d6 dihydrochloride (SKF 104864A-d6 dihydrochloride) is the deuterium labeled Topotecan dihydrochloride. 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-126373S
-
|
|
|
SN-38 glucuronide-d5 (SN-38G-d5) is the deuterium labeled SN-38 glucuronide (HY-126373). SN-38 glucuronide is an inactive metabolite of the anticancer active molecule Irinotecan (HY-16562) and has toxic effects on the gastrointestinal tract. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer.
|
-
-
- HY-13704S2
-
|
|
|
SN-38- 13C6 (7-Ethyl-10-hydroxycamptothecin- 13C6) is the 13C-labeled SN-38 (HY-13704). SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 can bind to RPL15. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254) .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-134723
-
|
|
|
DBCO
ADC Synthesis
|
|
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.
|
-
- HY-160788
-
|
|
|
DBCO
|
|
DBCO-β-Glu-PEG12-Exatecan (Compound 107) is an inhibitor for topoisomerase I. DBCO-β-Glu-PEG12-Exatecan can be used as a Drug-Linker Conjugate for ADC molecule .
|
-
- HY-164792
-
|
|
|
DBCO
|
|
DBCO-PEG3-VC-Exatecan (compound 25) is a Drug-Linker Conjugate for ADC. DBCO-PEG3-VC-Exatecan contains the ADC linker (DBCO-PEG3-VC) and a DNA topoisomerase I inhibitor Exatecan (HY-13631) .
|
-
- HY-173625
-
|
|
|
Alkynes
|
|
P5(PEG12)-VC-PAB-Exatecan (LP3) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG12)-VC-PAB-Exatecan can be used for the research of tumor .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-185370
-
|
Pegylated liposomal doxorubicin; Liposomal doxorubicin; Doxorubicin hydrochloride liposome
|
|
Liposome
|
|
Doxorubicin liposome is a liposome-encapsulated form of doxorubicin hydrochloride (HY-15142). Doxorubicin hydrochloride, a cytotoxic anthracycline antibiotic, is a potent human DNA topoisomerase I and topoisomerase II inhibitor. Compared to traditional doxorubicin, liposome encapsulation reduces its cardiotoxicity and prolongs its circulation time, thus enabling it to effectively target tumor tissue.
|
-
- HY-185371
-
|
Irinotecan hydrochlorid liposomee; Liposomal irinotecan
|
|
Liposome
|
|
Irinotecan liposome is a liposome-encapsulated form of Irinotecan hydrochlorid (HY-16562A) (a topoisomerase I inhibitor). Compared with Irinotecan, Irinotecan liposome enhances antitumor activity, reduces drug release rate, and avoids neutropenia.
|
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-13631AG
-
|
DX8951f
|
ADC Payload
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 .
|
-
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent:
![NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT](http://file.medchemexpress.com/product_pic/hy-148819.gif)
![NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride](http://file.medchemexpress.com/product_pic/hy-148819a.gif)
![Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT](http://file.medchemexpress.com/product_pic/hy-148820.gif)
![Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan](http://file.medchemexpress.com/product_pic/hy-173634.gif)
