S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin with a Kd of 0.93 μM and inhibts microtubule polymerization. S-methyl DM1 potently suppresses microtubule dynamic instability and has anticancer effects[1][2].
Dacarbazine(DTIC-Dome; DTIC) is an antineoplastic agent. It has significant activity against melanomas.Target: Nucleoside antimetabolite/analogApproved: May 1975Dacarbazine (DTIC) is the only single-agent approved by the Food and Drug Administration for treating metastatic melanoma. With DTIC as single agent, an approximately 20% objective response rate can be achieved with median response duration of 5 to 6 months and complete response rates of 5% [1]. Dacarbazine (DTIC) has activity in advanced previously untreated pancreatic islet cell tumors [2]. In the intent-to-treat population, median survival time was 7.7 months for patients treated with temozolomide and 6.4 months for those treated with DTIC (hazards ratio, 1.18; 95% confidence interval [CI], 0.92 to 1.52). Median PFS time was significantly longer in the temozolomide-treated group (1.9 months) than in the DTIC-treated group (1.5 months) (P = .012; hazards ratio, 1.37; 95% CI, 1.07 to 1.75) [3].
USP30 inhibitor 11 is a selective and potent ubiquitin specific peptidase 30 (USP30) inhibitor with an IC50 of 0.01 µΜ, the example 83 extracted from patent WO2017009650A1. USP30 inhibitor 11 is used for the study of cancer and conditions involving mitochondrial dysfunction[1].
Palmitic acid-d4 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
DMTr-FNA-C(Bz)Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC50 of 0.6 nM)[1].
RAD51-IN-5 is a potent inhibitor of RAD51. RAD51 is a eukaryote gene. RAD51-IN-5 has the potential for the research of conditions involving mitochondrial defects (extracted from patent WO2021164746A1, compound 3)[1].
2-Amino-1-β-D-ribofuranosyl-4(1H)-pyrimidinone is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
HA-100 dihydrochloride is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 dihydrochloride also used as a ROCK inhibitor[1][2].
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model[1].
eIF4A3-IN-6 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), such as eIF4AI and eIF4AII. eIF4A3-IN-6 has the potential for the research of eIF4A dependent diseases, including the research of cancer (extracted from patent US20170145026A1)[1].
HDAC-IN-40 is a potent alkoxyamide-based HDAC inhibitor with Ki values of 60 nM and 30 nM for HDAC2 and HDAC6, respectively. HDAC-IN-40 had antitumor effects[1].
Irinotecan-d10 ((+)-Irinotecan-d10) hydrochloride is the deuterium labeled Irinotecan. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex[1][2].
5-Benzylamino carbonyl-3’-O-acetyl-2’-O-methyluridine is a thymidine analogue. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
2-Iodoadenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Calenduloside E (CE) is a natural pentacyclic triterpenoid saponin extracted from Aralia elata. Calenduloside E (CE) has anti-apoptotic potent by targeting heat shock protein 90 (Hsp90)[1].
BAY-4931 is a potent, covalent and selective PPARγ inverse-agonist with an IC50 of 0.17 nM[1].
DDO-5936 is a potent and specific Hsp90-Cdc37 PPI inhibitor. DDO-5936 can be used for the research of colorectal cancer[1].
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model[1][2].
ABC1183 is a potent, selective, orally active GSK3α/β and CDK9 inhibitor with IC50 of 327/657 nM and 321 nM (CDK9/cyclin T1), shows growth inhibitory activity against a broad panel of cancer cell lines; decreases cell survival through G2/M arrest and modulates oncogenic signaling through changes in GSK3, GS and β-catenin phosphorylation and MCL1 expression; suppresses tumor growth and inflammation-driven gastrointestinal disease symptoms without organ or hematological toxicity in vivo.
CDK8-IN-10 (compound 2) is a potent, selective cyclin-dependent kinase (CDK8) inhibitor with an IC50 value of 8.25 nM. CDK8-IN-10 can be used for research of cancer[1].
BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay.
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition[1][2].
8-Methyladenosine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Folinic acid (Leucovorin) calcium hydrate is a biological folic acid and is generally administered along with Methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity[1].
hDHODH-IN-1 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor. hDHODH-IN-1 has anti-inflammatory effect[1].
ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity[1].
Topoisomerase II inhibitor 14 (compound 2f) is a potent inhibtor of Topoisomerase II, with anticancer activity. Topoisomerase II inhibitor 14 induces apoptosis, and arrests cell cycle at S phase. Topoisomerase II inhibitor 14 exhibits antioxidant effect and decreases the level of GSH, MDA, and NO[1].
(2’,3’,5’-Tri-O-acetyl)uridine 5-carboxylic acid is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
8-Benzyloxy-3’-deoxyguanosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].