Topo I Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S3898 Hydroxy Camptothecine

Hydroxy Camptothecine (10-Hydroxycamptothecin, Hydroxycamptothecine) is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.

S0093 Genz-644282

Genz-644282 is a non-camptothecin topoisomerase I (Topo I) inhibitor that demonstrates potent cytotoxic activity with a median IC50 of 1.2 nM (range 0.2 nM-21.9 nM). Genz-644282 can be used in cancer research.

Selective Topo I, IC50: 1.2 nM
S1231 Topotecan (NSC609699) HCl

Topotecan HCl (NSC609699, Nogitecan, SKFS 104864A) is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.

Selective Topo I (MCF-7 Luc cells), IC50: 13 nM; Topo I (DU-145 Luc cells), IC50: 2 nM
S1288 Camptothecin (NSC-100880)

Camptothecin (NSC-100880, CPT, Campathecin, (S)-(+)-Camptothecin) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2.

Selective Topo I, IC50: 0.68 μM
S3603 Betulinic acid

Betulinic acid (ALS-357, Lupatic acid, Betulic acid), a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Betulinic acid acts as a new activator of NF-kB.Phase 1/2.

Selective Eukaryotic topoisomerase I, IC50: 5 μM
S9321 Topotecan

Topotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.

S4908 SN-38

SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.

S2423 (S)-10-Hydroxycamptothecin

(S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity.

S6631 Belotecan (CKD-602) hydrochloride

Belotecan (CKD-602) is a potent DNA topoisomerase I inhibitor that exerts a clinical anticancer effect on various types of tumor.

S2288 Rubitecan

Rubitecan (9-NC, 9-Nitro-camptothecin, Partaject Orathecin, Partaject rubitecan, RFS 2000) is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral camptothecin with antitumour activity.

S7261 Beta-Lapachone

Beta-Lapachone (β-Lapachone, ARQ-501) is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.

S2653 9-amino-CPT (9-Aminocamptothecin)

9-amino-CPT (9-Aminocamptothecin, 9-AC, Aminocamptothecin, 9-amino-20(S)-camptothecin) is a Topoisomerase I inhibitor with potent anticancer activities. 9-amino-CPT (9-Aminocamptothecin) is an active, water-insoluble derivative of camptothecin.

S5026 Irinotecan hydrochloride

Irinotecan (CPT-11, (+)-Irinotecan) hydrochloride is an inhibitor of Topoisomerase I (Topo I) that exhibits cytotoxicity in LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.

S1198 Irinotecan (CPT-11)

Irinotecan (CPT-11, (+)-Irinotecan) is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.

S6747 SW-044248

SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells.

S5111 7-Ethylcamptothecin

7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition.

S2217 Irinotecan (CPT-11) HCl Trihydrate

Irinotecan (CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1.

S1327 Ellagic acid

Ellagic acid (Elagostasine, Gallogen) has antiproliferative and antioxidant property.

S2271 Berberine chloride (NSC 646666)

Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation