CDK6/9-IN-1 (compound 66) is an oral available and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively[1].
2’-O,4’-C-Methyleneuridine (Compound 15a) is a bicyclic nucleoside.
SNX-2112 is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively.
Maytansinol inhibits microtubule assembly and induces microtubule disassembly in vitro.Target: Microtubule/Tubulinin vitro: Maytansinol disrupts the mitotic spindle and prevents mitotic exit in Drosophila. Maytansinol reduces the growth and/or survival of HCT116 cells in a dose-dependent manner and that the effect was more severe for p53+/+ than for p53-/- cells at both low and high doses. Maytansinol inhibits the growth of HCT116 human colon cancer cells. Maytansinol induces apoptosis in imaginal discs of wild-type larvae but not p53 mutant larvae. This parallels the finding in human HCT116 cells, in which Maytansinol was more effective when p53 was present, at least at some doses. Maytansinol induces apoptosis in imaginal discs of wild-type larvae but not p53 mutant larvae at 24 hours after exposure to drug.
2′-Deoxy-5-methylisocytidine 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].
3’-Deoxy-N6-isopentenyl adenosine 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].
4'-Bromo-resveratrol is a potent and dual inhibitor Sirtuin-1 and Sirtuin-3. 4'-Bromo-resveratrol inhibits melanoma cell growth through mitochondrial metabolic reprogramming. 4'-Bromo-resveratrol imparts antiproliferative effects in melanoma cells through a metabolic reprogramming and affecting the cell cycle and apoptosis signaling[1].
Cdc7-IN-19 (compound 1-1) is a potent CDC7 inhibitor with an IC50 of 1.49 nM[1].
γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin (HY-19610) and β-Amanitin (HY-125586)[1].
Abacavir hydrochloride is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir hydrochloride can inhibits the replication of HIV. Abacavir hydrochloride shows anticancer activity in prostate cancer cell lines. Abacavir hydrochloride can trespass the blood-brain-barrier and suppresses telomerase activity[1][2][3].
8-Azaguanosine 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].
CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research[1].
HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has inhibitory activity against pre-miR-21 RNA. HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has the potential for the research of neoplastic disease such as cancer and especially cancers expressing miR-21 (extracted from patent WO2021087084A1, compound 25)[1].
Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.
Methylnitronitrosoguanidine (MNNG) is an alkylating agent with toxic and mutagenic effects[1].
DUBs-IN-2 is a potent deubiquitinase inhibitor with an IC50 of 0.28 μM for USP8.
Ribonuclease H is an enzyme degrading the RNA moiety of DNA-RNA hybrids[1].
2’-beta-C-Methyl-4-thiouridine 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].
5-(2,3,5-Tri-O-benzyl-beta-D-ribofuranosyl)-3-methyl-2-benzyloxypyridine 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].
CDK5 inhibitor 20-223 (CP 668863) potent, selective, ATP-competitive CDK2/5 inhibitor with IC50 of 6.0 and 8.8 nM for CDK2/CyclinE and CDK5/p35, with little to no activity against CDK1/4/6/7/9; decreases pRB (S807/811) and pFAK (S732) levels in CRC cell lines, effectively blocks the kinase activity of CDK2 and CDK5 in multiple CRC cell lines; reduces migration of CRC cells, reduces cell growth in a panel of human CRC cell lines with mean IC50 of 362 nM; effectively slows tumor progression in mice models.
LUF6283 is a potent and orally active HCA(2) partial agonist, with a Ki of 0.55 µM. LUF6283 can achieve the beneficial lipid lowering effect of niacin without producing the unwanted cutaneous flushing side effect[1].
USP8-IN-1 is a USP8 inhibitor with an IC50 of 1.9 μM. USP8-IN-1 inhibits H1975 cell growth with a GI50 of 82.04 μM (CN111138358A; U10)[1].
5-Bromo-2',3',5'-tri-O-acetyluridine diacetate 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].
6-O-Methylinosine is a hypoxanthine analogue. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia[1][2].
Adenine is a purine derivative and a nucleobase with a variety of roles in biochemistry. Target: Nucleoside antimetabolite/analogAdenine is a nucleobase with a variety of roles in biochemistry including cellular respiration, in the form of both the energy-rich adenosine triphosphate (ATP) and the cofactors nicotinamide adenine dinucleotide (NAD) and flavin adenine dinucleotide (FAD), andprotein synthesis, as a chemical component of DNA and RNA. The shape of adenine is complementary to either thymine in DNA or uracil in RNA.In older literature, adenine was sometimes called Vitamin B4. It is no longer considered a true vitamin or part of the Vitamin B complex. However, two B vitamins, niacin and riboflavin, bind with adenine to form the essential cofactors nicotinamide adenine dinucleotide (NAD) and flavin adenine dinucleotide (FAD), respectively. Hermann Emil Fischer was one of the early scientists to study adenine. Experiments performed in 1961 by Joan Oró have shown that a large quantity of adenine can be synthesized from the polymerization of ammonia with fivehydrogen cyanide (HCN) molecules in aqueous solution, whether this has implications for the origin of life on Earth is under debate.
Casein Kinase 2 Substrate Peptide is a common CK2 substrate peptide. Casein Kinase 2 Substrate Peptide is synthesized with its C-terminus conjugated to 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid (EDANS). Casein Kinase 2 Substrate Peptide can be used for protein kinase CK2 activity determination[1].
2BAct (eIF2B activator 2BAct) is a novel, highly selective, CNS-permeable small molecule eIF2B activator with EC50 of 33 nM in cell-based reporter assays; 2BAct normalized body weight gain and prevented motor deficits in male R191H mice, prevented myelin loss and reactive gliosis in the brain and spinal cord of R191H mice; also prevented ISR induction in the cerebellum and spinal cord of Eif2b5R132H/R132H mice, prevented all measures of pathology and normalizes the transcriptome and proteome of Vanishing White Matter (VWM) mice.
5’-Azido-5’-deoxy-2’-O-methyl-5-methyluridine 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].
(S)-Trichostatin A ((S)-TSA) 是一种 HDAC6 选择性抑制剂，对斑马鱼 HDAC6 和人 HDAC6 的 IC50 值分别为 9.88 nM和 11.1 nM。(S)-Trichostatin A 弱抑制其他人 HDAC。
3’-dC(Bz)-2’-phosphor amidite 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].