Mps1-IN-1 dihydrochloride is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM[1].
Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor. Zoliflodacin has potent in vitro antibacterial activity against Gram-positive and Gram-negative organisms, including S. aureus with the MIC90 of 0.25 μg/mL.
3,4-Dihydro-3-oxo-4-β-D-ribofuranosyl-2-pyrazinecarboxamide 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].
3’-Deoxy-3’-flluoro-3-deazauridine 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].
CAY10410 (11-Oxo-prosta-5Z), a 15d-PGJ2 analog, is a potent PPARγ agonist. CAY10410 has the ability to activate PPARγ in human B cells without killing B lymphocytes[1].
2’-Deoxy-N3-methylcytidine hydriodide 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].
OSIP-486823 is a novel microtubule-interfering agent with distinct biological effects on both protein kinase G (PKG) and microtubules.
Inixaciclib is a potent CDK inhibitor, that can be used to research anticancer.
IBU-DC Phosphoramidite is used for synthesis of oligonucleotides[1].
6-O-Methyl Guanosine is a modified nucleoside[1]. 6-O-Methyl Guanosine (6-methylguanosine) inhibit colony-forming ability in a malignant xeroderma pigmentosum cell line[2].
Oxolinic acid is a potent inhibitor of DNA gyrase and DNA synthesis, lead to DNA cleavage when extracted chromosomes are incubated with sodium dodecyl sulfate.
Sirt1/2-IN-3 (compound PS9) is a dual inhibitor of SIRT1/2 with IC50s of 1.4 μM (SIRT1) and 2.0 μM (SIRT2), respsectivley. Sirt1/2-IN-3 completely blocks p53 deacetylation, and increase of p53 and α-tubulin acetylation. Sirt1/2-IN-3 induces apoptosis and shows anti-proliferation activity against human leukemia cell lines[1].
Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC50s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation[1].
L-Guanosine is the L-configuration of Guanosine (HY-N0097). Guanosine is a purine nucleoside with anti-herpesvirus activity[1][2].
eIF4A3-IN-13 (compound 75) is a silvestrol (HY-13251) analogue. eIF4A3-IN-13 interferes the assembling of eIF4F translation complex with EC50s of 0.6, 15 and 0.4 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-13 can be used for the research of human cancer pathogenesis[1].
Alatrofloxacin, the parenteral prodrug of Trovafloxacin, is a fluoronaphthyridone which contains an L-alanyl-L-alanyl salt. Alatrofloxacin functions similar to other fluoroquinolone antibiotics in that it not only has antibiotic activity to kill invading organisms by interfering with DNA synthesis, it possesses immunosuppressive activity[1].
Edaglitazone is a potent, selective and orally active PPARγ agonist, with EC50s of 35.6 nM and 1053 nM for PPARα and PPARγ, respectively. Edaglitazone displays antiplatelet, antidiabetic and anti-hyperglycemic activity[1][2][3].
Sirt1/2-IN-2 (compound hsa55) is a dual inhibitor of SIRT1/2 with IC50s of 1.8 μM (SIRT1) and 2.4 μM (SIRT2), respsectivley. Sirt1/2-IN-2 completely blocks p53 deacetylation, and increase of p53 and α-tubulin acetylation. Sirt1/2-IN-2 induces apoptosis and shows anti-proliferation activity against human leukemia cell lines[1].
2’-Deoxy-2’-fluoro-N3-[(pyrid-4-yl)methyl]-beta-D-arabinouridine 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].
7,8-Dihydro-8-oxo-7-propargyl-3’-deoxy guanosine 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].
DNL343 is a brain-penetrating activator of eukaryotic initiation factor 2B (eIF2B) that inhibits the abnormal integrated stress response (ISR). DNL343 inhibits ISR activity in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 has inhibitory potential in studies of vanishing white matter disease (VWMD) driven by eIF2B LOF and chronic ISR activation[1].
Rac-Nedisertib (Rac-M3814) is a racemate of Nedisertib, a potent DNA-PK inhibitor, with an IC50 of <3 nM[1].
USP7-IN-7 (compound 124) is a USP7 inhibitor with an IC50 value ＜10 nM. USP7-IN-7 shows cytotoxicity against p53-mutant cancer cell lines, p53 wild-type blood cancer and neuroblastoma cell lines with low nanomolar values. USP7-IN-7 can be used for cancer research[1].
AQ4 is a topoisomerase II inhibitor and DNA intercalator as a chemically stable cytotoxic agent in many human tumor lines[1].
m-Carboxycinnamic acid bishydroxamide is a potent HDAC inhibitor, exhibiting ID50 values of 10 and 70 nM in vitro for HDAC1 and HDAC3, respectively[1]. m-Carboxycinnamic acid bishydroxamide also induces apoptosis and suppresses tumor growth[2].
CDK7/12-IN-1 is a selective CDK7/12 inhibitor with IC50s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth[1].
DPQ is a potent PARP-1 inhibitor. DPQ can reduce the N-methyl-d-aspartate (NMDA)-induced PARP activation, restoring ATP to near control levels and significantly attenuating neuronal injury in the severe NMDA exposure model. DPQ can be used for researching neuroprotection[1].
Taq DNA polymerase is a thermostable DNA polymerase that can be used in PCR[1].
Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent[1][2][3][4].
AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.