Campathecin is a potent DNA enzyme topoisomerase I inhibitor, with an IC50 of 679 nM.
Paclitaxel is a potent anticancer medication which can promote microtubule (MT) assembly, inhibit MT depolymerization, and change MT dynamics required for mitosis and cell proliferation.
Aeruginosin 865, isolated from terrestrial cyanobacterium Nostoc sp. Lukešová 30/93, is the first aeruginosin-type peptide containing both a fatty acid and a carbohydrate moiety. Aeruginosin 865 inhibits translocation of NF-kB to the nucleus. Aeruginosin 865 has anti-inflammatory effect[1]
Aldoxorubicin (INNO-206) is an albumin-binding prodrug of doxorubicin, which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in in murine tumor models.
CC-885-CH2-PEG1-NH-CH3 is a neoDegrader that can be used in the synthesis of Antibody neoDegrader Conjugate (AnDC)[1][2].
Agrochelin, an alkaloid cytotoxic antibiotic, is produced by the fermentation of a marine Agrobacterium sp. Agrochelin has cytotoxic activity in tumor cell lines[1].
Tubulysin A(TubA) is a myxobacterial product that can function as an antiangiogenic agent in many in vitro assays; anti-microtubule, anti-mitotic, an apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative.IC50 value: Target: microtubuleTubulysin A is a novel antibiotic, which is anti-microtubule, anti-mitotic, apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative. Tubulysins are cytotoxic peptides, which include 9 members (A-I). Tubulysin A has potential application as an anticancer agent. It arrests cells in the G2/M phase. Tubulysin A inhibits polymerization more efficiently than vinblastine and induces depolymerization of isolated microtubules. Tubulysin A has potent cytostatic effects on various tumor cell lines with IC50 in the picomolar range.
Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin[1][2][3].
SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent[1].
Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
Hemiasterlin derivative-1 is a hemiasterlin derivative. Hemiasterlin derivative-1 can be used for the synthesis of the Antibody-drug conjugate (ADC)[1].
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).
DM1-SMe is an unconjugated form of the Maytansinoid in IMGN901. DM1-SMe is about 3-10-fold more potent than the parent drug Maytansine, with IC50s ranging from 0.003 to 0.01 nM for DM1-SMe in a panel of human tumor cell lines[1].
DOXO-EMCH is a 6-maleimidocaproyl hydrazone derivative of Doxorubicin, is an albumin binding prodrug.
Py-MPB-amino-C3-PBD is a cytotoxic agent comprised non-alkylating group. Py-MPB-amino-C3-PBD acts as the payload for ADCs. Antimicrobial activity[1].
MMAF hydrochloride is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM.
Maytansinoid DM4 is a thiol-containing maytansine derivative with highly potent cytotoxicity. Maytansinoid DM4 can be used as a cytotoxic moiety of ADC[1][2].
Puwainaphycin F, a cyanobacterial cyclic lipopeptide, is a moderate cytotoxin isolated from the soil cyanobacterium Cylindrospermum alatosporum C24/89. Puwainaphycin F causes necrotic cell death to mammalian cells via cell membrane permeabilization and subsequent unusual actin relocalization[1].
Doxorubicin hydrochloride is a cytotoxic anthracycline antibiotic for the treatment of multiple cancers. The possible mechanisms by which doxorubicin acts in the cancer cell are intercalation into DNA and disruption of topoisomerase-II-mediated DNA repair.
alpha-Amanitin is the principal toxin of several deadly poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.
NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (compound I) is a topoisomerase I inhibitor, which can be delivered to cells through conjugated antibody targeting, and has good ADC activity in vivo and in vitro[1].
Clezutoclax is a potent payload and also a Bcl-XL inhibitor. Clezutoclax can be used in the synthesis of antibody-drug conjugates (ADCs)[1].
Sandramycin ia a cyclic depsipeptide antibiotic isolated from cultured broth of a Nocardioides sp. Sandramycin is also a DNA intercalator that potently binds DNA and is an ADC cytotoxin. Sandramycin is active against Gram-positive bacteria and has potent antitumor activity[1][2][3].
ε-Amanitin, a cyclic peptide isolated from a variety of mushroom species, potently binds to and inhibits the activity of RNA polymerase II[1][2].
Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A (PA; HY-114936) and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts[1][2].
Maytansinoid B is a kind of ADC Cytotoxin. Maytansinoid B can be used to conjugates with antibodies to form Antibody-Drug Conjugates (ADCs). Maytansinoids are known as antimitotic agents, binding to tubulin and inhibiting microtubule assembly. Maytansinoids induces G2/M arrest in the cell cycle to induce apoptosis[1][2].
(rac)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer[1][2].
MMAF sodium (Monomethylauristatin F sodium) is an antitubulin agent that inhibit cell division; attenuates its cytotoxic activity compared to MMAE. MMAF sodium is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
Doxorubicin is a cytotoxic anthracycline antibiotic for the treatment of multiple cancers. The possible mechanisms by which doxorubicin acts in the cancer cell are intercalation into DNA and disruption of topoisomerase-II-mediated DNA repair.
Duocarmycin A, which is one of well-known antitumor antibiotics, efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels[1].