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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6-Chloro-2-hydroxy-9-(2',3',5'-tri-O-acetyl-b-D-ribofuranosyl)purine

6-Chloro-2-hydroxy-9-(2',3',5'-tri-O-acetyl-β-D-ribofuranosyl)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: 161923-50-8
  • MF: C16H17ClN4O8
  • MW: 428.78
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Vc-MMAD

Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulin inhibitor (MMAD), Vc-MMAD is an antibody drug conjugate.IC50 Valu: N/ATarget: tubulin; ADCsMonomethyl auristatin D (MMAD), a potent tubulin inhibitor, is a toxin payload and antibody drug conjugate.For comparison purposes, the ADC A1 -mc-MMAD and/or A1 -vc-MMAD were used. The linker payload, mc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) was conjugated to the A1 anti-5T4 monoclonal antibody through a cysteine residue at a ratio of approximately 4 drug moieties per antibody molecule. The linker payload mc- Val-Cit-PABA-MMAD or vc-MMAD (maleimidocapronic -valine-citruline-p- aminobenzyloxycarbonyl- monomethylauristatin-D) was conjugated to the A1 anti-5T4 monoclonal antibody through a cysteine residue at a ratio of approximately 4 drug moieties per antibody molecule (Antibody-drug conjugates Patent: WO 2013068874 A1).

  • CAS Number: 1401963-17-4
  • MF: C70H104N12O14S
  • MW: 1369.712
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 1370.7±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 782.8±34.3 °C

DMT-2'-O-Methyladenosine phosphoramidite

DMT-2'-O-Methyladenosine phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.

  • CAS Number: 138906-75-9
  • MF: C41H50N7O7P
  • MW: 783.85
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3,5-Bis-O-(2,4-dichlorobenzyl)adenosine

3,5-Bis-O-(2,4-dichlorobenzyl)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: 2095417-71-1
  • MF: C24H21Cl4N5O4
  • MW: 585.3
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Vorinostat(SAHA)

Vorinostat is a potent and orally available inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV ), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively.

  • CAS Number: 149647-78-9
  • MF: C14H20N2O3
  • MW: 264.320
  • Catalog: Autophagy
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 161-162°C
  • Flash Point: N/A

3-Deoxy-1,2-O-isopropylidene-5-p-toluoyl-a-D-glycero-pent-3-enofuranose

3-Deoxy-1,2-O-isopropylidene-5-p-toluoyl-a-D-glycero-pent-3-enofuranose 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: 75096-63-8
  • MF: C16H18O5
  • MW: 290.31
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CDK4/6-IN-14

CDK4/6-IN-14 is a potent and highly selective CDK4 and CDK6 (CDK) inhibitor with IC50s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases[1].

  • CAS Number: 2699091-15-9
  • MF: C24H27ClFN7O
  • MW: 483.97
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Auristatin F

Auristatin F is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAF analog and cytotoxin in Antibody-drug conjugates.

  • CAS Number: 163768-50-1
  • MF: C40H67N5O8
  • MW: 745.989
  • Catalog: ADC Cytotoxin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 894.4±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 494.7±34.3 °C

Z26395438

Z26395438 (compound 1) is a potent Sirtuin-1 inhibitor, with an IC50 value of 1.6 μM[1].

  • CAS Number: 2803-63-6
  • MF: C17H15FN2O
  • MW: 282.31
  • Catalog: Sirtuin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BTB1

BTB-1 is a potent, selective and reversible mitotic motor protein Kif18A inhibitor with an IC50 of 1.69 μM.

  • CAS Number: 86030-08-2
  • MF: C12H8ClNO4S
  • MW: 297.71400
  • Catalog: Microtubule/Tubulin
  • Density: 1.476g/cm3
  • Boiling Point: 471.2ºC at 760mmHg
  • Melting Point: 115ºC
  • Flash Point: 238.8ºC

2’-Chloro-N6-(4-trifluoromethyl)benzyl adenosine

2’-Chloro-N6-(4-trifluoromethyl)benzyl 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].

  • CAS Number: 722515-03-9
  • MF: C18H17ClF3N5O4
  • MW: 459.81
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CP-67804

CP-67804 is a quinolone derivative, is a topoisomerase II-targeted agent. CP-67804 effectively enhances DNA cleavage mediated by eukaryotic topoisomerase II. CP-67804 has potential as an antineoplastic agent[1].

  • CAS Number: 103978-08-1
  • MF: C18H13F2NO4
  • MW: 345.29700
  • Catalog: Topoisomerase
  • Density: 1.456g/cm3
  • Boiling Point: 526.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 272.2ºC

Amphethinile

Amphethinile is an anti-tubulin agent. The affinity constant for the association (Ka) of Amphethinile with tubulin is 1.3 μM.

  • CAS Number: 91531-98-5
  • MF: C15H11N3S
  • MW: 265.33300
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DHPS-IN-1

DHPS-IN-1, with the best DHPS inhibitory potency (IC50 = 0.014 μM), exhibits excellent inhibition against melanoma cells.

  • CAS Number: 2643300-54-1
  • MF: C17H13BrClN3O2
  • MW: 406.66
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Duocarmycin GA

Duocarmycin GA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin GA can be used against multi-drug resistant cell lines.

  • CAS Number: 1613286-59-1
  • MF: C26H25ClN4O3
  • MW: 476.95
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’-O-Acetyl-N4-benzoyl-5’-O-DMT arabinocytidine 3’-O-phosphoramidite

2’-O-Acetyl-N4-benzoyl-5’-O-DMT arabinocytidine 3’-O-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: 675573-97-4
  • MF: C48H54N5O10P
  • MW: 891.94
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Deoxycytidine triphosphate trisodium salt

Deoxycytidine triphosphate trisodium salt (dCTP trisodium salt) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate trisodium salt has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing[1][2][3].

  • CAS Number: 109909-44-6
  • MF: C9H13N3Na3O13P3
  • MW: 533.102
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

APE1 Inhibitor III

APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells[1].

  • CAS Number: 524708-03-0
  • MF: C19H21N3OS2
  • MW: 371.52000
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CDK7/9-IN-1

CDK7/9-IN-1 is a cyclin-dependent kinases 7/9 (CDK7/9) inhibitor. CDK7/9-IN-1 selectively inhibits CDK7 over CDK9. CDK7/9-IN-1 inhibits CDK7 with IC50s of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. CDK7/9-IN-1 inhibits CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation. CDK7/9-IN-1 can be used for the research of cancer[1].

  • CAS Number: 2747919-19-1
  • MF: C24H32F3N5O2
  • MW: 479.54
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BRCA1-IN-1

BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor with IC50 and Ki of 0.53 μM and 0.71 μM, respecrively.

  • CAS Number: 1622262-74-1
  • MF: C27H33F2N4O6P
  • MW: 578.54
  • Catalog: PARP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mating Factor α (1-6) acetate salt

Mating Factor α (1-6) is a mating factor produced by α-mating type cells of Saccharomyces cerevisiae and an acts as an inhibitor of the initiation of DNA synthesis in the cells[1].

  • CAS Number: 65418-88-4
  • MF: C45H59N11O8
  • MW: 882.01900
  • Catalog: DNA/RNA Synthesis
  • Density: 1.32g/cm3
  • Boiling Point: 1395.3ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 797.6ºC

Tacaciclib

Tacaciclib is a CDK inhibitor, antineoplastic effect[1].

  • CAS Number: 2768774-66-7
  • MF: C30H36N6O3
  • MW: 528.65
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CHK1 inhibitor

CHK1 inhibitor is an inhibitor of CHK1.

  • CAS Number: 2097938-64-0
  • MF: C17H21BrN4O
  • MW: 377.28
  • Catalog: Checkpoint Kinase (Chk)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Kira8 Hydrochloride

Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM[1].

  • CAS Number: 2250019-92-0
  • MF: C31H30Cl2N6O3S
  • MW: 637.58
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’-Deoxy-2’-fluoro-N1-methyl inosine

2’-Deoxy-2’-fluoro-N1-methyl inosine 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: 2376610-64-7
  • MF: C11H13FN4O4
  • MW: 284.24
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

7-cyano-7-deazaguanosine

7-Cyano-7-deazaguanosine 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: 61210-21-7
  • MF: C12H13N5O5
  • MW: 307.26
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5'-DMTr-dG(iBu)-Methyl phosphonamidite

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

  • CAS Number: 115131-08-3
  • MF: C42H53N6O7P
  • MW: 784.88
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cdc7-IN-6

Cdc7-IN-6 (compound I-D) is a potent Cdc7 kinase inhibitor (IC50=4 nM), extracted from patent WO2019165473A1, compound I- D, has anti-tumor activity[1].

  • CAS Number: 1402057-88-8
  • MF: C21H22F3N5O4
  • MW: 465.43
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

EPI-001

EPI-001 is a selective inhibitor of Androgen Receptor (AR), and it can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of 6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 exhibits anti-tumor activity in vitro and in vivo[1][2].

  • CAS Number: 227947-06-0
  • MF: C21H27ClO5
  • MW: 394.889
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 601.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 317.2±31.5 °C

N6-Benzoyl-9-β-D-arabinofuranosyladenine

N6-Benzoyl-9-β-D-arabinofuranosyladenine 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: 79896-97-2
  • MF: C17H17N5O5
  • MW: 371.35
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A