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.


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2-Chloro-N6-methyladenosine

2-Chloro-N6-methyladenosine 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: 13406-50-3
  • MF: C11H14ClN5O4
  • MW: 315.71
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mulnitorsen

Mulnitorsen is an antisense non-coding mitochondrial RNA (ASncmtRNA) synthesis reducer. Mulnitorsen is an antitumor agent[1].

  • CAS Number: 2576358-63-7
  • MF: C172H217N74O82P17S17
  • MW: 5704.66
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GRL 0617

GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro)/deubiquitinase, with an IC50 of 0.6 μM, and with a Ki of 0.49 μM[1].

  • CAS Number: 1093070-16-6
  • MF: C20H20N2O
  • MW: 304.38600
  • Catalog: SARS-CoV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

COH29

COH29 is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.

  • CAS Number: 1190932-38-7
  • MF: C22H16N2O5S
  • MW: 420.43800
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dideoxycytidinene

Dideoxycytidinene (2′,3′-Didehydro-2′,3′-dideoxycytidine) 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: 7481-88-1
  • MF: C9H11N3O3
  • MW: 209.20
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-Aminosalicylic acid-d3

5-Aminosalicylic acid-d3 is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[1][2][3][4].

  • CAS Number: 1309283-32-6
  • MF: C7H4D3NO3
  • MW: 156.154
  • Catalog: PAK
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 403.9±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 198.1±27.3 °C

2’-β-C-Methyl-5-methoxyuridine

2’-β-C-Methyl-5-methoxyuridine 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: 2072145-45-8
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Vincristine Sulfate

Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM.

  • CAS Number: 2068-78-2
  • MF: C46H58N4O14S
  • MW: 923.036
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: 273-281 °C
  • Melting Point: 300 °C
  • Flash Point: N/A

N6-Bz-5’-O-DMTr-2’-O-hexadecanyl adenosine 3’-CED phosphoramidite

N6-Bz-5’-O-DMTr-2’-O-hexadecanyl adenosine 3’-CED phosphoramidite 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: 2382942-35-8
  • MF: C63H84N7O8P
  • MW: 1098.36
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DM4

DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody drug conjugate.

  • CAS Number: 796073-69-3
  • MF: C38H54ClN3O10S
  • MW: 780.36700
  • Catalog: Microtubule/Tubulin
  • Density: 1.29±0.1 g/cm3
  • Boiling Point: 943.2±65.0 °C
  • Melting Point: 185-187 °C (decomp)
  • Flash Point: N/A

Kenpaullone

Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively.

  • CAS Number: 142273-20-9
  • MF: C16H11BrN2O
  • MW: 327.175
  • Catalog: CDK
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 613.0±45.0 °C at 760 mmHg
  • Melting Point: >300ºC (dec.)
  • Flash Point: 324.5±28.7 °C

3’-Deoxy-3’-fluoro-N6,N6-dimethyladenosine

3’-Deoxy-3’-fluoro-N6,N6-dimethyladenosine 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: 122654-28-8
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JH-RE-06

JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 sensitizes mouse and human cell lines to Cisplatin, and suppresses tumor progression in mice and prolongs animal survival[1].

  • CAS Number: 1361227-90-8
  • MF: C20H16Cl3N3O4
  • MW: 468.72
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CMPD101

CMPD101, is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively)[1].

  • CAS Number: 865608-11-3
  • MF: C24H21F3N6O
  • MW: 466.458
  • Catalog: ROCK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LY2606368 (dihydrochloride)

Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a potent and selective ATP competitive inhibitor of the Chk1 protein kinase, with IC50s of <1 nM and 8 nM for CHK1 and CHK2, respectively, and a Ki of 0.9 nM against purified CHK1.

  • CAS Number: 1234015-54-3
  • MF: C18H21Cl2N7O2
  • MW: 438.31
  • Catalog: Checkpoint Kinase (Chk)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4′,5′-Didehydro-5′-deoxy-2′-O-methyluridine

4′,5′-Didehydro-5′-deoxy-2′-O-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].

  • CAS Number: 1848223-48-2
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-N-Boc-aminomethyluridine

5-N-Boc-aminomethyluridine 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: 2305415-73-8
  • MF: C15H23N3O8
  • MW: 373.36
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

EGFR/HER2/CDK9-IN-2

EGFR/HER2/CDK9-IN-2 (Compound 9) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 145.35, 129.07, and 117.13 nM, respectively. EGFR/HER2/CDK9-IN-2 exhibits remarkable antitumor activity[1].

  • CAS Number: 1180924-34-8
  • MF: C23H20N4O5S2
  • MW: 496.56
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Seconeolitsine

Seconeolitsine, an antibiotic, and is an inhibitor of targeting topoisomerase I (TopA). Seconeolitsine also is a new antimicrobial agent that can inhibit S. pneumoniae growth. Seconeolitsine can inhibit TopA relaxation activity with an IC50 value of 17 μM. Seconeolitsine can be used for the research of S. pneumoniae infections resistant to other antibiotics[1].

  • CAS Number: 2650074-56-7
  • MF: C19H17NO4
  • MW: 323.34
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3'-Azido-3'-deoxyadenosine

3'-Azido-3'-deoxyadenosine 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: 58699-62-0
  • MF: C10H12N8O3
  • MW: 292.25
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(13,13,14,14,15,15,16,16,16-2H9)Hexadecanoic acid

Palmitic acid-d9 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: 1173022-49-5
  • MF: C16H23D9O2
  • MW: 265.48
  • Catalog: HSP
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 340.6±5.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 154.1±12.5 °C

WC-3035

Sarecycline is an orally effective narrow-spectrum tetracycline derivative antibiotic. Sarecycline has anti-inflammatory activity. Sarecycline inhibits the activity of Gram-positive bacteria and several types of keratobacterium acnes. Sarecycline interferes with tRNA accommodation and tethers mRNA to the 70S ribosome. Sarecycline can be used to study moderate to severe acne[1][2][3][4][5][6].

  • CAS Number: 1035654-66-0
  • MF: C24H29N3O8
  • MW: 487.50200
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Guanine-13C

Guanine-13C is the 13C labeled Guanine[1]. Guanine (2-Aminohypoxanthine) is one of the fundamental components of nucleic acids (DNA and RNA). Guanine is a purine derivative, consisting of a fused pyrimidine-imidazole ring system with conjugated double bonds.

  • CAS Number: 201489-20-5
  • MF: C413CH5N5O
  • MW: 152.12
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SY-1365

SY-1365 is a highly selective covalent inhibitor of CDK7. SY-1365 possesses therapeutic potential in both hematological and solid tumors[1].

  • CAS Number: 1816989-16-8
  • MF: C31H35ClN8O2
  • MW: 587.12
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

bio-THZ1

bio-THZ1 is a biotinylated version of THZ1 and binds irreversibly to CDK7. THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM[1].

  • CAS Number: 1604811-14-4
  • MF: C52H65ClN12O8S
  • MW: 1053.67
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Amino-6-allyl thio-9-(beta-D-ribofuranosyl)-9H-purine

2-Amino-6-allyl thio-9-(beta-D-ribofuranosyl)-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: 92104-54-6
  • MF: C13H17N5O4S
  • MW: 339.37
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5'-DMTr-dA(Bz)-Methyl phosphonamidite

5'-DMTr-dA(Bz)-Methyl phosphonamidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.

  • CAS Number: 114079-05-9
  • MF: C45H51N6O6P
  • MW: 802.90
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3-(2-Pyridinylmethyl)uridine

N3-[(Pyrid-2-yl)methyl]uridine 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: 1427676-15-0
  • MF: C15H17N3O6
  • MW: 335.31
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AV-153 free base

AV-153 free base, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 free base intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 free base interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 free base has anti-cancer activity[1][2][3].

  • CAS Number: 19350-66-4
  • MF: C14H19NO6
  • MW: 297.30400
  • Catalog: DNA/RNA Synthesis
  • Density: 1.23g/cm3
  • Boiling Point: 450.5ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 226.3ºC

Pemafibrate

Pemafibrate is a potent PPARα agonist, with EC50s of 1 nM, 1.10 μM and 1.58 μM for h-PPARα, h-PPARγ and h-PPARδ, respectively, and possesses lipid-lowering effect.

  • CAS Number: 848259-27-8
  • MF: C28H30N2O6
  • MW: 490.54800
  • Catalog: PPAR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A