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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RAD51-IN-7

RAD51-IN-7 is a potent inhibitor of RAD51. RAD51 is a eukaryote gene. RAD51-IN-7 has the potential for the research of conditions involving mitochondrial defects (extracted from patent WO2021164746A1, compound 71)[1].

  • CAS Number: 2690368-52-4
  • MF: C25H31N5O4S2
  • MW: 529.67
  • Catalog: RAD51
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-N-Acetyl-3’-amino-3’-deoxyuridine

3’-N-Acetyl-3’-amino-3’-deoxyuridine 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: 2305415-89-6
  • MF: C11H15N3O6
  • MW: 285.25
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CNDAC

CNDAC is a major metabolite of oral drug sapacitabine, and a nucleoside analog.

  • CAS Number: 135598-68-4
  • MF: C10H12N4O4
  • MW: 252.22700
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Kira8

Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α’s RNase[1].

  • CAS Number: 1630086-20-2
  • MF: C31H29ClN6O3S
  • MW: 601.12
  • Catalog: IRE1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cdc7-IN-11

Cdc7-IN-11 is a highly potent Cdc7 inhibitor with IC50≤1 nM. Cdc7-IN-11 can be used for researching proliferative diseases[1].

  • CAS Number: 2649409-19-6
  • MF: C20H22F2N4O2S
  • MW: 420.48
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cucurbitacin D

Cucurbitacin D is an active component in Cucurbita texana, disrupts interactions between Hsp90 and two co-chaperones, Cdc37 and p23. Cucurbitacin D prevents Hsp90 client (Her2, Raf, Cdk6, pAkt) maturation without induction of the heat shock response. Anti-cancer activity[1].

  • CAS Number: 3877-86-9
  • MF: C30H44O7
  • MW: 516.666
  • Catalog: HSP
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 684.0±55.0 °C at 760 mmHg
  • Melting Point: 151-152ºC
  • Flash Point: 381.4±28.0 °C

Zagotenemab

Zagotenemab (LY3303560) is a humanised anti-tau antibody that selectively binds and neutralises tau deposits in the brain. Zagotenemab can be used in Alzheimer's disease research[1].

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

3’-β-Amino-2’,3’-dideoxy-5’-O-trityl-5-methyl uridine

3’-β-Amino-2’,3’-dideoxy-5’-O-trityl-5-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: 204688-08-4
  • MF: C29H29N3O4
  • MW: 483.6
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N1-Cyclopropylmethylpseudouridine

N1-Cyclopropylmethylpseudouridine 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: 1613530-18-9
  • MF: C13H18N2O6
  • MW: 298.29
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Eleutherobin

Eleutherobin is a potent β-microtubule inhibitor with an IC50 value of 2 μM. Eleutherobin can be isolated from a marine soft coral. Eleutherobin has cytotoxic activity against cancer cells with similar potency to that of Paclitaxel (HY-B0015). Anticancer activity[1][2].

  • CAS Number: 174545-76-7
  • MF: C35H48N2O10
  • MW: 656.76300
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-Methyl-4’-thiocytidine

5-Methyl-4’-thiocytidine 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: 1312295-87-6
  • MF: C10H15N3O4S
  • MW: 273.31
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Chebulinic acid

Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.

  • CAS Number: 18942-26-2
  • MF: C41H32O27
  • MW: 956.677
  • Catalog: DNA/RNA Synthesis
  • Density: 2.0±0.1 g/cm3
  • Boiling Point: 1460.0±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 437.2±27.8 °C

DUB-IN-7

DUB-IN-7 (compound 43) is a Deubiquitinating enzymes (DUBs) inhibitor. DUB-IN-7 can be used in the study of diseases mediated by dysregulated JAK2 activity, such as leukemia[1].

  • CAS Number: 2894064-79-8
  • MF: C17H19N5O
  • MW: 309.37
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Gemcitabine HCl

Gemcitabine hydrochloride is a DNA synthesis inhibitor with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM in BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells, respectively.

  • CAS Number: 122111-03-9
  • MF: C9H12ClF2N3O4
  • MW: 299.659
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: 482.7ºC at 760 mmHg
  • Melting Point: >250°C dec.
  • Flash Point: N/A

PERK-IN-2

PERK-IN-2 is a potent PERK inhibitor with an IC50 of 0.2 nM[1].

  • CAS Number: 1337531-83-5
  • MF: C23H18F3N5O
  • MW: 437.42
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’,3’,5’-Tri-O-benzoyl-2’-β-C-methyl-5-methoxy uridine

2’,3’,5’-Tri-O-benzoyl-2’-β-C-methyl-5-methoxy 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: 2072145-79-8
  • MF: C32H28N2O10
  • MW: 600.57
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin inhibitor 11

Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis[1].

  • CAS Number: 2366260-33-3
  • MF: C22H23N3O3S
  • MW: 409.50
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Apoptozole

Apoptozole is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.

  • CAS Number: 1054543-47-3
  • MF: C33H25F6N3O3
  • MW: 625.56000
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Kihadanin B

Kihadanin B is a citrus limonoid that can be purified from the peels of immature Citrus unshiu. Kihadanin B suppresses adipogenesis through repression of the Akt-FOXO1-PPARγ axis in 3T3-L1 adipocytes[1].

  • CAS Number: 73793-68-7
  • MF: C26H30O9
  • MW: 486.51100
  • Catalog: PPAR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

UNII:SHY3J1BBQ6

Bromochloroacetonitrile is a by-product of the chlorine disinfection of water containing natural organic material. Bromochloroacetonitrile possesses direct acting mutagenic activity and is capable of inducing DNA strand breakage[1].

  • CAS Number: 83463-62-1
  • MF: C2HBrClN
  • MW: 154.393
  • Catalog: DNA/RNA Synthesis
  • Density: 1.9±0.1 g/cm3
  • Boiling Point: 121.1±20.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 27.1±21.8 °C

2’-Deoxy-N3-methylcytidine

2’-Deoxy-N3-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: 5040-21-1
  • MF: C10H15N3O4
  • MW: 241.24
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin polymerization-IN-27

Tubulin polymerization-IN-27 (compound 5j) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-27 can arrest cell cycle at G2/M phase and induce apoptosis[1].

  • CAS Number: 2462030-32-4
  • MF: C22H20N2O2
  • MW: 344.41
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ricolinostat (ACY-1215)

Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.

  • CAS Number: 1316214-52-4
  • MF: C24H27N5O3
  • MW: 433.503
  • Catalog: HDAC
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-ap-2'-dCTP·xTEA

5-Propargylamino-dCTP is a nucleoside molecule extracted from patent US9035035B2, compound dCTP-PA. 5-Propargylamino-dCTP can conjugate to molecular markers for use in nucleic acid labeling or sequence analysis[1].

  • CAS Number: 115899-39-3
  • MF: C12H19N4O13P3
  • MW: 520.219
  • Catalog: DNA/RNA Synthesis
  • Density: 2.2±0.1 g/cm3
  • Boiling Point: 836.0±75.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 459.4±37.1 °C

A-3 hydrochloride

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively[1].

  • CAS Number: 78957-85-4
  • MF: C12H14Cl2N2O2S
  • MW: 321.22300
  • Catalog: Casein Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 173-176ºC
  • Flash Point: N/A

Fmoc-Ala-OH-13C3

Fmoc-Ala-OH-13C3 is a 13C-labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-ind

  • CAS Number: 765259-05-0
  • MF: C1513C3H17NO4
  • MW: 314.31
  • Catalog: PPAR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N4-Bz-2'-OMe-rC

N4-Benzoyl-2’-O-methylcytidine 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: 52571-45-6
  • MF: C17H19N3O6
  • MW: 361.35
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.49g/cm3
  • Boiling Point: N/A
  • Melting Point: 174-175ºC
  • Flash Point: N/A

3’-Azido-3’-deoxy-5-fluorouridine

3’-Azido-3’-deoxy-5-fluorouridine 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: 307520-05-4
  • MF: C9H10FN5O5
  • MW: 287.20
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HBV-IN-23

HBV-IN-23 (Compound 5k) is an inhibitor of HBV DNA replication with an IC50 of 0.58 µM. HBV-IN-23 inhibits HBV DNA replication in both drug sensitive and resistant HBV strains. HBV-IN-23 shows anti-hepatocellular carcinoma cell (HCC) activities. HBV-IN-23 induces HepG2 cells apoptosis[1].

  • CAS Number: 2413649-89-3
  • MF: C25H27N3O3S
  • MW: 449.57
  • Catalog: HBV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DMT-LOCMEC(BZ)AMIDITE 0.25G 89 SINGLE

DMT-locMeC(bz) phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.

  • CAS Number: 206055-82-5
  • MF: C48H54N5O9P
  • MW: 875.94
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A