Cell Cycle includes many processes necessary for successful self-replication, and consists of DNA synthesis (S) and mitosis (M) phases separated by gap phases in the order G1–S–G2–M. S phase and M phase are usually separated by gap phases called G1 and G2, when cell-cycle progression can be regulated by various intracellular and extracellular signals. In order to move from one phase of its life cycle to the next, a cell must pass through numerous checkpoints. At each checkpoint, specialized proteins determine whether the necessary conditions exist. Progression through G1 phase is controlled by pRB proteins, and phosphorylation of pRB proteins by CDKs releases E2F factors, promoting the transition to S phase. The G2/M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1/S transition, many proteins, such Wee1, PLK1 and cdc25, is involved the regulation of this process. The best-understood checkpoints are those activated by DNA damage and problems with DNA replication.

DNA damage response (DDR) is a series of regulatory events including DNA damage, cell-cycle arrest, regulation of DNA replication, and repair or bypass of DNA damage to ensure the maintenance of genomic stability and cell viability. Genome instability arises if cells initiate mitosis when chromosomes are only partially replicated or are damaged by a double-strand DNA break (DSB). To prevent cells with damaged DNA from entering mitosis, ATR inhibits cyclin B/Cdk1 activation by stimulating the Cdk1 inhibitory kinase Wee1 and inhibiting Cdc25C via Chk1, besides, ATM and ATR also initiate DNA repair by phosphorylating several other substrates.

In cancer cells, the cell cycle regulators as well as other elements of the DDR pathway have been found to protect tumor cells from different stresses and to promote tumor progression. Thus, cell cycle proteins that directly regulate cell cycle progression (such as CDKs), as well as checkpoint kinases, Aurora kinases and PLKs, are promising targets in cancer therapy.

References:
[1] Rhind N, et al. Cold Spring Harb Perspect Biol. 2012 Oct; 4(10): a005942.
[2] Duronio RJ, et al. Cold Spring Harb Perspect Biol. 2013 Mar; 5(3): a008904.
[3] Liu W, et al. Mol Cancer. 2017 Mar 14;16(1):60.
[4] Ghelli Luserna di Rora' A, et al. J Hematol Oncol. 2017 Mar 29;10(1):77.


Anti-infection >
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Palmitic acid-9,10-d2

Palmitic acid-9,10-d2 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].

  • CAS Number: 78387-70-9
  • MF: C16H30D2O2
  • MW: 258.44
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

isodiospyrin

Isodiospyrin, a natural dimeric naphthoquinone, is a human DNA topoisomerase I (Topoisomerase) inhibitor. Isodiospyrin can prevent both DNA relaxation and kinase activities of human topoisomerase I. Isodiospyrin shows anticancer, antibacterial and antifungal activities[1][2][3].

  • CAS Number: 20175-84-2
  • MF: C22H14O6
  • MW: 374.343
  • Catalog: Bacterial
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 712.0±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 398.3±29.4 °C

6-Amino-1,2-dihydro-2-β-D-ribofuranosyl-4H-pyrazolo[3,4-d]pyrimidin-4-one

6-Amino-1,2-dihydro-2-β-D-ribofuranosyl-4H-pyrazolo[3,4-d]pyrimidin-4-one 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].

  • CAS Number: 85426-86-4
  • MF: C10H13N5O5
  • MW: 283.24
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Palmitic acid-d2-3

Palmitic acid-d2-3 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA 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].

  • CAS Number: 83293-32-7
  • MF: C16H30D2O2
  • MW: 258.44
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ML216

ML216(CID-49852229) is a potent inhibitor of the DNA unwinding activity of BLM helicase; showing similar IC50s of 3.0 and 0.97 μM for full length BLM and BLM636–1298 respectively.IC50 value: 3.0/0.97 uM(Full length/636–1298 BLM)Target: BLM helicase inhibitorML216 shows cell-based activity, and can induce sister chromatid exchanges, enhance to the toxicity of aphidicolin and exert anti-proliferative activity in cells expressing BLM, but not in those lacking BLM.

  • CAS Number: 1430213-30-1
  • MF: C15H9F4N5OS
  • MW: 383.323
  • Catalog: DNA/RNA Synthesis
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Phthalazinone pyrazole

Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells[1][2].

  • CAS Number: 880487-62-7
  • MF: C18H15N5O
  • MW: 317.345
  • Catalog: Aurora Kinase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 557.7±52.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 291.1±30.7 °C

2’-Amino-2’-deoxy-5-methyl uridine

2’-Amino-2’-deoxy-5-methyl uridine 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].

  • CAS Number: 869729-38-4
  • MF: C10H15N3O5
  • MW: 257.24
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

c-Myc inhibitor 7

c-Myc inhibitor 7 is a c-Myc inhibitor and a multiple target protein degrader. c-Myc inhibitor 7 effective degrades c-MYC, CK1α, GSPT1 and IKZF1/2/3 proteins in a variety of tumor cells. c-Myc inhibitor 7 can be used for c-Myc high expression related disease research, such as cancer, cardiovascular and cerebrovascular diseases, and viral infection[1].

  • CAS Number: 2883535-99-5
  • MF: C35H30N6O5
  • MW: 614.65
  • Catalog: c-Myc
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1,2-Di-O-acetyl-5-O-benzoyl-3-deoxy-3-fluoro-D-ribofuranose

1,2-Di-O-acetyl-5-O-benzoyl-3-deoxy-3-fluoro-D-ribofuranose is a ribofuranose nucleoside analogue.

  • CAS Number: 159099-24-8
  • MF: C16H17FO7
  • MW: 340.30
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 422.9±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 202.2±23.6 °C

5-[5-[(Z)-[1-(3-carboxyphenyl)-3-methyl-5-oxopyrazol-4-ylidene]methyl]furan-2-yl]-2-chlorobenzoic acid

TDRL-X80 is a potent inhibitor of xeroderma pigmentosum group A (XPA) protein. TDRL-X80 inhibits XPA’s DNA binding activity. TDRL-X80 exhibits activity against single, double, and Cisplatin-damaged DNA with IC50s of 18, 20, and 29 μM in fluorescence polarization (FP) analyses , and with IC50s of 21, 39, and 28 in ELISA Analysis[1].

  • CAS Number: 292065-64-6
  • MF: C23H15ClN2O6
  • MW: 450.82800
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

FIT-039

FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.

  • CAS Number: 1113044-49-7
  • MF: C17H18FN3S
  • MW: 315.408
  • Catalog: CMV
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 460.4±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 232.2±31.5 °C

USP1-IN-5

USP1-IN-5 (compound 10) is a USP1 inhibitor (IC50<50 nM). USP1-IN-5 also inhibits MDA-MB-436 cells with IC50 <50 nM[1].

  • CAS Number: 2925547-94-8
  • MF: C27H23F3N8O
  • MW: 532.52
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Icariin

Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.

  • CAS Number: 489-32-7
  • MF: C33H40O15
  • MW: 676.662
  • Catalog: Autophagy
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 948.5±65.0 °C at 760 mmHg
  • Melting Point: 223-225ºC
  • Flash Point: 300.9±27.8 °C

5-Iminodaunorubicin

5-Iminodaunorubicin is a quinone-modified anthracycline that retains antitumor activity[1]. 5-Iminodaunorubicin produces protein-concealed DNA strand breaks in cancer cells[2].

  • CAS Number: 72983-78-9
  • MF: C27H30N2O9
  • MW: 526.54
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TN-16

TN-16 is a potent inhibitor of microtubule polymerization with IC50 of 0.4-1.7 µM[1].

  • CAS Number: 33016-12-5
  • MF: C19H18N2O2
  • MW: 306.35800
  • Catalog: Microtubule/Tubulin
  • Density: 1.249g/cm3
  • Boiling Point: 532.7ºC at 760 mmHg
  • Melting Point: 182-185 °C
  • Flash Point: 195.5ºC

Adavosertib (MK-1775)

Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor with an IC50 of 5.2 nM.

  • CAS Number: 955365-80-7
  • MF: C27H32N8O2
  • MW: 500.595
  • Catalog: Wee1
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 723.8±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 391.5±35.7 °C

2'-Deoxyguanosine 5'-(Tetrahydrogen Triphosphate)

dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP[1].

  • CAS Number: 2564-35-4
  • MF: C10H16N5O13P3
  • MW: 507.18
  • Catalog: DNA/RNA Synthesis
  • Density: 2.63g/cm3
  • Boiling Point: 989.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 552.2ºC

CAY10760

Homologous recombination-IN-1 is a novel RAD51-BRCA2 protein-protein interaction inhibitor (EC50=19 μM). Homologous recombination-IN-1 can interfere with homologous recombination[1].

  • CAS Number: 391889-85-3
  • MF: C28H24ClN3O3
  • MW: 485.961
  • Catalog: RAD51
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N6-Benzoyl-2'-O-tert-butyldimethylsilyl-3'-O-DMT-adenosine

N6-Benzoyl-2'-O-tert-butyldimethylsilyl-3'-O-DMT-adenosine 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].

  • CAS Number: 1214886-17-5
  • MF: C44H49N5O7Si
  • MW: 787.97
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TCMDC-124283

2-Fluoroadenine is a toxic purine bases. 2-Fluoroadenine has toxicity in nonproliferating and proliferating tumor cells. 2-Fluoroadenine can be used for researching anticancer[1].

  • CAS Number: 700-49-2
  • MF: C5H4FN5
  • MW: 153.12
  • Catalog: DNA/RNA Synthesis
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: 676.9±58.0 °C at 760 mmHg
  • Melting Point: >350 °C(lit.)
  • Flash Point: 363.2±32.3 °C

ACX-362E

ACX-362E is an orally available DNA polymerase IIIC (pol IIIC) inhibitor, acts as an antimicrobial agent to treat Gram-positive infections, with a MIC50 of 2 μg/mL for C. difficile. ACX-362E displays very potent in vitro and in vivo activities against broad spectrum of C. difficile pathogens[1].

  • CAS Number: 1275582-97-2
  • MF: C18H20Cl2N6O2
  • MW: 423.30
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

360A iodide

360A iodide is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.

  • CAS Number: 737763-37-0
  • MF: C27H23I2N5O2
  • MW: 703.31
  • Catalog: G-quadruplex
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4’-Cyanouridine

4’-Cyanouridine is a uridine analogue. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].

  • CAS Number: 232589-05-8
  • MF: C10H11N3O6
  • MW: 269.21
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DMT-LNA-G phosphoramidite

DMT-LNA-G phosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.

  • CAS Number: 207131-17-7
  • MF: C41H48N7O8P
  • MW: 797.84
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

eIF4A3-IN-17

eIF4A3-IN-17 (compound 61) is a silvestrol (HY-13251) analogue. eIF4A3-IN-17 interferes the assembling of eIF4F translation complex with EC50s of 0.9, 15 and 1.8 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-17 can be used for the research of human cancer pathogenesis[1].

  • CAS Number: 1402931-75-2
  • MF: C28H25NO7
  • MW: 487.50
  • Catalog: Eukaryotic Initiation Factor (eIF)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

7-Propargyl-7,8-dihydro-8-oxo-9-(β-D-xylofuranosyl)guanine

7-Propargyl-7,8-dihydro-8-oxo-9-(β-D-xylofuranosyl)guanine 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].

  • CAS Number: 2389988-31-0
  • MF: C13H15N5O6
  • MW: 337.29
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’-O-Acetyl-5’-O-benzoyl-3’-O-methyl-5-methyl uridine

2’-O-Acetyl-5’-O-benzoyl-3’-O-methyl-5-methyl uridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].

  • CAS Number: 2305415-91-0
  • MF: C20H22N2O8
  • MW: 418.40
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Votoplam

Votoplam is a gene splicing modulator, used to inhibit Huntington's disease[1].

  • CAS Number: 2407849-89-0
  • MF: C21H25N9O
  • MW: 419.48
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HDAC1/2-IN-3

HDAC1/2-IN-3 is a HDAC1 and HDAC2 inhibitor with IC50 values 0-5 and 5-10 nM, respectively.

  • CAS Number: 2121516-17-2
  • MF: C24H25N5OS
  • MW: 431.55
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3'-Amino-3'-deoxyuridine

3’-Amino-3’-deoxyuridine 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].

  • CAS Number: 70580-90-4
  • MF: C9H13N3O5
  • MW: 243.22
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A