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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3’,5’-Di-O-acetyl-2’-deoxy-N3-methyl uridine

3’,5’-Di-O-acetyl-2’-deoxy-N3-methyl uridine 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: 2305416-14-0
  • MF: C14H18N2O7
  • MW: 326.30
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-AMINO-6-CHLORO-9-(3,5-DI-O-(P-TOLUOYL)-BETA-D-2-DEOXYRIBOFURNANOSYL)PURINE

2-Amino-6-chloropurine-9-beta-D-(2’-deoxy-3’,5’-di-O-(p-toluoyl))riboside 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: 35095-93-3
  • MF: C26H24ClN5O5
  • MW: 521.95
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-Deoxy-3’-fluoro-5-methylcytidine

3’-Deoxy-3’-fluoro-5-methylcytidine 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: 847650-07-1
  • MF: C10H14FN3O4
  • MW: 259.23
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

L82

L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM). L82 shows anti-proliferative activity to breast cancer cells[1][2].

  • CAS Number: 329227-30-7
  • MF: C11H8ClN5O4
  • MW: 309.67
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N4-Benzoyl-7'-OH-N-trityl Morpholino cytosine

N4-Benzoyl-7’-OH-N-trityl morpholino cytosine 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: 125515-31-3
  • MF: C35H32N4O4
  • MW: 572.65
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1,N6-Ethenoadenosine

1,N6-Ethenoadenosine 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: 39007-51-7
  • MF: C12H13N5O4
  • MW: 291.26
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.99g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3,7,4'-trihydroxyflavone

3,7,4'-Trihydroxyflavone, isolated from Rhus javanica var. roxburghiana, is a flavonoid with DNA strand-scission activity[1].

  • CAS Number: 2034-65-3
  • MF: C15H10O5
  • MW: 270.24
  • Catalog: DNA/RNA Synthesis
  • Density: 1.579g/cm3
  • Boiling Point: 539.7ºC at 760mmHg
  • Melting Point: 310-311ºC
  • Flash Point: 210.6ºC

2'-OMe-ibu-G Phosphoramidite

2'-OMe-G(ibu) Phosphoramidite is a modified phosphoramidite monomer, which can be used for the oligonucleotide synthesis.

  • CAS Number: 150780-67-9
  • MF: C45H56N7O9P
  • MW: 869.941
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S-(N-PhenethylthiocarbaMoyl)-L-cysteine

S-(N-PhenethylthiocarbaMoyl)-L-cysteine, a anticarcinogenic agent, has antileukaemic activity with a GC50 value of 336 nM. S-(N-PhenethylthiocarbaMoyl)-L-cysteine inhibits DNA synthesis in HL60 cells [1].

  • CAS Number: 53330-02-2
  • MF: C12H16N2O2S2
  • MW: 284.40
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

hypoxanthine-9-beta-d-arabinofuranoside

Arabinosylhypoxanthine 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: 7013-16-3
  • MF: C10H12N4O5
  • MW: 268.23
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.08g/cm3
  • Boiling Point: 732.8ºC at 760 mmHg
  • Melting Point: 259-260 °C (lit.)
  • Flash Point: 397ºC

Xanthopterin Hydrate

Xanthopterin hydrate, an unconjugated pteridine compound, is the main component of the yellow granule in the Oriental hornet bear wings, produces a characteristic excitation/emission maximum at 386/456 nm[2]. Xanthopterin hydrate(XPT) causes renal growth and hypertrophy in rat[1].Xanthopterin hydrate inhibits RNA synthesis[4].

  • CAS Number: 5979-01-1
  • MF: C6H7N5O3
  • MW: 197.15100
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: 458.7ºC at 760 mmHg
  • Melting Point: >300 °C(lit.)
  • Flash Point: 231.2ºC

Exoenzyme C3, clostridium botulinum

Exoenzyme C3, clostridium botulinum is a promising agent to inactivate RhoA in neurons due to preventing the detrimental effect of active Rho in the recovery of injured neuronal systems. Exoenzyme C3, clostridium botulinum is used for the study of post-traumatic neuro-regeneration[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cdc7-IN-8

Cdc7-IN-8 is a potent inhibitor of Cdc7. Cdc7 is a serine/threonine kinase which activates MCM promotion by phosphorylating the microchromosome maintenance protein (MCM protein), an important element of the DNA replication initiator. Cdc7-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021032170A1, compound 1-1/1-2)[1].

  • CAS Number: 2606780-38-3
  • MF: C19H21N5O2
  • MW: 351.40
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N4-BENZOYL-3'-DEOXYCYTIDINE

N4-Benzoyl-3’-deoxycytidine 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: 161110-00-5
  • MF: C16H17N3O5
  • MW: 331.32
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.503 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

sulfo-DGN462 sodium

sulfo-DGN462 sodium is degraded to DGN462 in culture medium and plasma. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML)[1].

  • CAS Number: 1401203-09-5
  • MF: C53H60N5NaO12S2
  • MW: 1046.19
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MMAF

MMAF (Monomethylauristatin F) is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM.

  • CAS Number: 745017-94-1
  • MF: C39H65N5O8
  • MW: 731.962
  • Catalog: ADC Cytotoxin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 896.8±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 496.2±34.3 °C

SIRT7 inhibitor 97491

SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway.[1].

  • CAS Number: 1807758-81-1
  • MF: C15H12ClN3O
  • MW: 285.73
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MSC 1094308

MSC1094308 is a reversible and allosteric inhibitor of the type II AAA ATPase human ubiquitin-directed unfoldase (VCP)/p97 and the type I AAA ATPase VPS4B, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively[1].

  • CAS Number: 2219320-08-6
  • MF: C29H29F3N2
  • MW: 462.55
  • Catalog: p97
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

xylocytidine

Xylocytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].

  • CAS Number: 3530-56-1
  • MF: C9H13N3O5
  • MW: 243.22
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Crotonoside

Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the treatment of AML[1].

  • CAS Number: 1818-71-9
  • MF: C10H13N5O5
  • MW: 283.241
  • Catalog: HDAC
  • Density: 2.3±0.1 g/cm3
  • Boiling Point: 831ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 456.4ºC

Cdc7-IN-3

Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle[1].

  • CAS Number: 1402057-87-7
  • MF: C20H22N4O5
  • MW: 398.41
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PAK1-IN-1

PAK1-IN-1 is a potent and selective PAK1 inhibitor with an IC50 of 9.8 nM. PAK1-IN-1 inhibits the migration and invasion of PAK1-related tumour cells in a dose-dependent manner[1].

  • CAS Number: 2485732-30-5
  • MF: C26H20ClN5O2
  • MW: 469.92
  • Catalog: PAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cotosudil

Cotosudil is a ROCK kinase inhibitor, which can be used for glaucoma or ocular hypertension research[1].

  • CAS Number: 1258833-31-6
  • MF: C16H21N3O2S
  • MW: 319.42
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Amino-6-chloro-9-(3-deoxy-beta-D-ribofuanosyl)-9H-purine

2-Amino-6-chloro-9-(3-deoxy-beta-D-ribofuanosyl)-9H-purine 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: 1055035-48-7
  • MF: C10H12ClN5O3
  • MW: 285.69
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.0±0.1 g/cm3
  • Boiling Point: 681.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 366.2±34.3 °C

2′-Deoxy-2′-fluoro-5-methyl-arabinocytidine

2′-Deoxy-2′-fluoro-5-methyl-arabinocytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].

  • CAS Number: 78636-53-0
  • MF: C10H14FN3O4
  • MW: 259.23
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.73 g/cm3
  • Boiling Point: 495.4ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 253.4ºC

ROCK2-IN-6 hydrochloride

ROCK2-IN-6 hydrochloride (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research[1].

  • CAS Number: 2762238-94-6
  • MF: C26H22ClF2N7O
  • MW: 521.95
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NCT-58

NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells[1].

  • CAS Number: 2411429-33-7
  • MF: C27H34N2O5
  • MW: 466.57
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

[5-(6-aminopurin-9-yl)-3-hydroxy-oxolan-2-yl]methylimino-imino-azanium

5′-Azido-2′,5′-dideoxyadenosine 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: 42204-43-3
  • MF: C10H12N8O2
  • MW: 276.25
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5’-Deoxy-5’-furfurylamino thymidine

5’-Deoxy-5’-furfurylamino thymidine 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: 2305416-15-1
  • MF: C15H19N3O5
  • MW: 321.33
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PERK-IN-6

PERK-IN-6 (Compound 5) is a PERK inhibitor with an IC50 of 2.5 nM[1].

  • CAS Number: 1337532-14-5
  • MF: C23H22N6O
  • MW: 398.46
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A