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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5’-O-TBDPS-5-methyl-2,2’-anhydrouridine

5’-O-TBDPS-5-methyl-2,2’-anhydrouridine 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: 171763-19-2
  • MF: C26H30N2O5Si
  • MW: 478.61
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Methoxypyrimidin-4-amine

2-O-Methylcytosine, an O-alkylated analogue a DNA adduct, is the damaged nucleobase[1].

  • CAS Number: 3289-47-2
  • MF: C5H7N3O
  • MW: 125.129
  • Catalog: DNA/RNA Synthesis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 294.4±32.0 °C at 760 mmHg
  • Melting Point: 167-171 °C
  • Flash Point: 131.9±25.1 °C

2’-O-Acetyl-5’-O-(p-toluoyl)-3’-deoxy-3’-fluoro-5-fluorouridine

2’-O-Acetyl-5’-O-(p-toluoyl)-3’-deoxy-3’-fluoro-5-fluorouridine 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: 2072145-63-0
  • MF: C19H18F2N2O7
  • MW: 424.35
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AT9283

AT9283 is a multitargeted kinase inhibitor which potently inhibits aurora kinase A/B, JAK2/3 (IC50=1.2 nM, 1.1 nM).

  • CAS Number: 896466-04-9
  • MF: C19H23N7O2
  • MW: 381.432
  • Catalog: Autophagy
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CMLD012612

CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity[1].

  • CAS Number: 2368900-35-8
  • MF: C31H33N3O7
  • MW: 559.61
  • Catalog: Eukaryotic Initiation Factor (eIF)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ZN-c3

ZN-c3 is an orally active, highly potent and selective Wee1 inhibitor (IC50=3.9 nM). ZN-c3 can be used for the research of cancer[1].

  • CAS Number: 2376146-48-2
  • MF: C29H34N8O2
  • MW: 526.63
  • Catalog: Wee1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BRD7586

BRD7586 is a cell-permeable small-molecule inhibitor of SpCas9. BRD7586 is the smallest known anti-CRISPR[1].

  • CAS Number: 895460-70-5
  • MF: C17H14ClN3O3S2
  • MW: 407.89436
  • Catalog: CRISPR/Cas9
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DMT-dC(bz) Phosphoramidite

DMT-dC(bz) Phosphoramidite is typically used in the synthesis of DNA[1].

  • CAS Number: 102212-98-6
  • MF: C46H52N5O8P
  • MW: 833.907
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N6-Benzoyl-2',3'-isopropylideneadenosine

N6-Benzoyl-2',3'-isopropylidene 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: 39947-04-1
  • MF: C20H21N5O5
  • MW: 411.41
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.58±0.1 g/cm3(Predicted)
  • Boiling Point: N/A
  • Melting Point: 144-146 °C
  • Flash Point: N/A

2’-Deoxy-N4,N4-dimethylcytidine

2’-Deoxy-N4,N4-dimethylcytidine 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: 53213-03-9
  • MF: C11H17N3O4
  • MW: 255.27
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 453.4±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 228.0±31.5 °C

LJ570

LJ570 is a PPARα/PPARγ dual agonist with EC50s of 1.05 and 0.12 μM, respectively[1].

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

Cyclapolin 9

Cyclapolin 9 is a potent, selective and ATP-competitive polo-like kinase 1 (PLK1) inhibitor with an IC50 of 500 nM. Cyclapolin 9 is inactive against other kinases[1][2].

  • CAS Number: 40533-25-3
  • MF: C9H4F3N3O4S
  • MW: 307.20600
  • Catalog: Polo-like Kinase (PLK)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Chlorambucil

Chlorambucil is an alkylating agent with antitumor activity.

  • CAS Number: 305-03-3
  • MF: C14H19Cl2NO2
  • MW: 304.212
  • Catalog: Peptides
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 460.1±40.0 °C at 760 mmHg
  • Melting Point: 64ºC
  • Flash Point: 232.1±27.3 °C

HDAC6-IN-4

HDAC6-IN-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity[1].

  • CAS Number: 2709103-20-6
  • MF: C30H38N2O5
  • MW: 506.63
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Casein kinase 1δ-IN-9

Casein kinase 1δ-IN-9 (compound 737) is a potent casein kinase 1δ (CK1δ/CK15) inhibitor. Casein kinase 1δ-IN-9 can be used for the research of neurodegenerative disorders such as Alzheimer's disease[1].

  • CAS Number: 854355-54-7
  • MF: C15H12ClN3
  • MW: 269.73
  • Catalog: Casein Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VCE-004.8

VCE-004.8, a semi-synthetic multitarget cannabinoquinoid, is a specific PPARγ and CB2 receptor dual agonist with potent anti-inflammatory activity[1]. VCE-004.8 inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. VCE-004.8 attenuates adipogenesis and prevents diet-induced obesity[2].

  • CAS Number: 1818428-24-8
  • MF: C28H35NO3
  • MW: 433.58
  • Catalog: PPAR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DNA Gyrase-IN-5

DNA Gyrase-IN-5 (Compound 8I-w) is a potent DNA gyrase inhibitor with an IC50 of 0.10 μM. DNA Gyrase-IN-5 shows antibacterial activities against wild type and drug-resistant strains[1].

  • CAS Number: 2417016-23-8
  • MF: C25H15BrClN5
  • MW: 500.78
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Chk1-IN-6

Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.

  • CAS Number: 2428423-77-0
  • MF: C16H18F3N7
  • MW: 365.36
  • Catalog: Checkpoint Kinase (Chk)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Colchicine

Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM.

  • CAS Number: 64-86-8
  • MF: C22H25NO6
  • MW: 399.437
  • Catalog: Autophagy
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 726.0±60.0 °C at 760 mmHg
  • Melting Point: 150-160 °C (dec.)(lit.)
  • Flash Point: 392.9±32.9 °C

Illudin S

Illudin S is a sesquiterpene toxin with strong anti-tumour and antiviral activities. Illudin S has genotoxic activities[1][2][3].

  • CAS Number: 1149-99-1
  • MF: C15H20O4
  • MW: 264.31700
  • Catalog: Apoptosis
  • Density: 1.34g/cm3
  • Boiling Point: 509.6ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 276.1ºC

(1S,9R)-Exatecan mesylate

(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research[1].

  • CAS Number: 2938875-54-6
  • MF: C25H26FN3O7S
  • MW: 531.55
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5'-DMT-2'-TBDMS-Ac-rC

5'-O-DMT-2'-O-TBDMS-Ac-rC is a modified nucleoside and can be used to synthesize DNA or RNA.

  • CAS Number: 121058-85-3
  • MF: C38H47N3O8Si
  • MW: 701.88100
  • Catalog: DNA/RNA Synthesis
  • Density: 1.19±0.1 g/cm3(Predicted)
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TLR7 agonist 11

TLR7 agonist 11 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: 2389988-36-5
  • MF: C14H17N5O8
  • MW: 383.31
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IU1

IU1 is a special Usp14 inhibitor with IC50 of 4-5 μM.

  • CAS Number: 314245-33-5
  • MF: C18H21FN2O
  • MW: 300.371
  • Catalog: Deubiquitinase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 437.0±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 218.1±28.7 °C

Vincristine-d3 sulfate

Vincristine-d3 (Leurocristine-d3) sulfate is the deuterium labeled 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[1][2].

  • CAS Number: 1246817-10-6
  • MF: C46H55D3N4O14S
  • MW: 926.05
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-Azido-3’-deoxy-5-fluoro-beta-L-uridine

3’-Azido-3’-deoxy-5-fluoro-beta-L-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: 2095417-40-4
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

RAD51-IN-3

RAD51-IN-3 is a Rad51 inhibitor extracted from patent WO2019051465A1, compound Example 66A[1].

  • CAS Number: 2301084-99-9
  • MF: C31H41N5O5S2
  • MW: 627.82
  • Catalog: RAD51
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Adenosine dialdehyde

Adenosine Dialdehyde is a purine nucleoside analogue and is an irreversible inhibitor of S-adenosylhomocysteine hydrolase (SAH) (IC50=40 nM). Adenosine Dialdehyde exhibits potent anti-tumor activity in vivo and can be used for the cancer research[1][2].

  • CAS Number: 34240-05-6
  • MF: C10H11N5O4
  • MW: 265.22500
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Camptothecin-20(S)-O-propionate

Camptothecin-20(S)-O-propionate (CZ48), the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor[1][2][3].

  • CAS Number: 194414-69-2
  • MF: C23H20N2O5
  • MW: 404.41500
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-Deoxy-3’-fluoroinosine

3’-Deoxy-3’-fluoroinosine 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: 117517-20-1
  • MF: C10H11FN4O4
  • MW: 270.22
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.0±0.1 g/cm3
  • Boiling Point: 682.1±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 366.3±34.3 °C