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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2,6-Diamino-9-(2-C-Methyl-β-D-ribofuranosyl)-9H-purine

2-Amino-2′-C-methyladenosine 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: 640725-73-1
  • MF: C11H16N6O4
  • MW: 296.28
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.0±0.1 g/cm3
  • Boiling Point: 754.6±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 410.2±35.7 °C

2′-β-C-Methyl-beta-D-6-methylpurine riboside

2′-β-C-Methyl-beta-D-6-methylpurine riboside 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: 2095417-06-2
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HDAC-IN-58

HDAC-IN-58 is a HDAC inhibitor. HDAC-IN-58 has HDAC6-specific inhibition activity with an IC50 value of 2.06 nM. HDAC-IN-58 can be used for the research of chronic diseases, including neurodegenerative and psychiatric conditions[1].

  • CAS Number: 2071224-39-8
  • MF: C16H13ClF2N4O3S
  • MW: 414.81
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SR-1277

SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer[1].

  • CAS Number: 1446715-47-4
  • MF: C21H19N9O3S
  • MW: 477.50
  • Catalog: Casein Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KX-01-191

KX-01-191, a Boronic Ester Precursor, is a potent PARP inhibitor[1].

  • CAS Number: 2211903-84-1
  • MF: C28H39N3OSn
  • MW: 552.34
  • Catalog: PARP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-O-(t-Butyldimethylsilyl)-2’-O-(2-methoxyethyl) uridine

3’-O-(t-Butyldimethylsilyl)-2’-O-(2-methoxyethyl) uridine is a uridine analog. 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: 1345716-52-0
  • MF: C19H34N2O7Si
  • MW: 430.57
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

9H-Purin-6-amine,9-(2-deoxy-b-D-threo-pentofuranosyl)-

9-(2-Deoxy-β-D-threo-pentofuranosyl)-9H-purin-6-amine 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: 13276-53-4
  • MF: C10H13N5O3
  • MW: 251.24
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.91g/cm3
  • Boiling Point: 627.2ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 333.1ºC

GGFG-amide-glycol-amide-Exatecan

GGFG-amide-glycol-amide-Exatecan (Intermediate 2) is an Exatecan (HY-13631) derivative and can be used in the synthesis of antibody-drug conjugates (ADCs)[1].

  • CAS Number: 2866301-18-8
  • MF: C43H47FN8O11
  • MW: 870.88
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Alpinetin

Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity[1].

  • CAS Number: 36052-37-6
  • MF: C16H14O4
  • MW: 270.280
  • Catalog: PPAR
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 494.9±45.0 °C at 760 mmHg
  • Melting Point: 223-224ºC
  • Flash Point: 188.8±22.2 °C

Estramustine phosphate sodium

Estramustine phosphate sodium is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.

  • CAS Number: 52205-73-9
  • MF: C23H30Cl2NNa2O6P
  • MW: 564.347
  • Catalog: Microtubule/Tubulin
  • Density: 1.253g/cm3
  • Boiling Point: 565.8ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 296ºC

NMS-P515

NMS-P515 is a potent and stereospecific PARP-1 inhibitor, with an IC50 of 27 nM in hela cells. Anti-tumor activity[1].

  • CAS Number: 1262395-13-0
  • MF: C21H29N3O2
  • MW: 355.47
  • Catalog: PARP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TP3011

TP3011 is a potent topoisomerase-1 inhibitor and is the active metabolite converted from TP3076 by aldehyde oxidase 1 (AOX1)[1]. TP3011 has robust anti-tumor activities against cancer cell lines[2].

  • CAS Number: 534605-74-8
  • MF: C26H26N4O5
  • MW: 474.51
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

17-GMB-APA-GA

17-GMB-APA-GA is an ADC Cytotoxin. 17-GMB-APA-GA is a potent HSP90 inhibitor and used for latent T. gondii infection research[1].

  • CAS Number: 256337-10-7
  • MF: C39H53N5O11
  • MW: 767.87
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PAK4-IN-1

PAK4-IN-1 (Compound 19) is a potent, selective, orally active PAK4 inhibitor with robust anti-tumor efficacy in vivo. PAK4-IN-1 is stable under both acidic and neutral conditions[1].

  • CAS Number: 2396529-58-9
  • MF: C26H30ClN7O5
  • MW: 556.01
  • Catalog: PAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cdc7-IN-13

Cdc7-IN-13 (compound 84) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-13 has the potential for the research of cancer[1].

  • CAS Number: 2764866-23-9
  • MF: C18H20N4O2S
  • MW: 356.44
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-(2-Hydroxyethyl)uridine

5-(2-Hydroxyethyl)uridine is a thymidine analogue. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].

  • CAS Number: 102691-28-1
  • MF: C11H16N2O7
  • MW: 288.25
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3'-O-tert-Butyldimethylsilyl-5'-O-DMT-N2-isobutyrylguanosine 2'-CE phosphoramidite

3'-TBDMS-ibu-rG Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.

  • CAS Number: 1445905-51-0
  • MF: C50H68N7O9PSi
  • MW: 970.18
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SR31527

SR31527 is a novel allosteric Kinesin-like protein KIFC1 inhibitor that inhibits microtubule-stimulated KIFC1 ATPase activity with IC50 of 6.6 uM, binds directly to KIFC1 with Kd of 25.4 nM; prevents bipolar clustering of extra centrosomes in TNBC cells and significantly reducesTNBC cell colony formation and viability (MDA-MB-231, BT549 and MDA-MB-435s cells IC50=20-30 uM), with less toxicity to normal fibroblasts.

  • CAS Number: 311814-78-5
  • MF: C15H14ClN3OS
  • MW: 319.807
  • Catalog: Kinesin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CFI-402257 hydrochloride

CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50s of 1.7 nM for TTK in vitro. CFI-402257 hydrochloride has anti-cancer activity[1].

  • CAS Number: 1610677-37-6
  • MF: C28H31ClN6O3
  • MW: 535.04
  • Catalog: Mps1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Deoxythymidine-5'-triphosphate-13C10,15N2 dilithium

Deoxythymidine-5'-triphosphate-13C10,15N2 (dTTP-13C10,15N2) dilithium is 13C and 15N-labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.

  • CAS Number: 2483830-18-6
  • MF: 13C10H15Li215N2O14P3
  • MW: 505.95
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1-bromo-2-(2-bromophenyl)disulfanyl-benzene

Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells[1].

  • CAS Number: 71112-91-9
  • MF: C12H8Br2S2
  • MW: 376.13000
  • Catalog: Microtubule/Tubulin
  • Density: 1.83g/cm3
  • Boiling Point: 386.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 187.8ºC

Cefminox sodium

Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity[1]. Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension[2].

  • CAS Number: 75498-96-3
  • MF: C16H20N7NaO7S3
  • MW: 541.557
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

RET-IN-19

RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research[1].

  • CAS Number: 2484919-71-1
  • MF: C28H28N6O4S
  • MW: 544.62
  • Catalog: Aurora Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’-Deoxy-2’-fluoro-4’-thio-β-D-arabinouridine

2’-Deoxy-2’-fluoro-4’-thio-β-D-arabinouridine 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: 941610-00-0
  • MF: C9H11FN2O4S
  • MW: 262.26
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-[(3,4,5-trimethoxyphenyl)methyl]pyrimidine-2,4-diamine hydrochloride

Trimethoprim hydrochloride is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim hydrochloride is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim hydrochloride has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim hydrochloride can inhibit infection of Influenza A virus in chick embryo when combinated with zinc[1][2][3][4].

  • CAS Number: 60834-30-2
  • MF: C14H19ClN4O3
  • MW: 326.77900
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: 526ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 271.9ºC

CDK2/4/6-IN-2

CDK2/4/6-IN-2 is a CKD2/4/6 inhibitor, with IC50 values less than 1 μM, 10 nM, 100 nM respectively[1].

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

Thailanstatin C

Thailanstatin C is a pre-mRNA splicing inhibitor (IC50= 6.84 μM) and antiproliferative agent from Burkholderia thailandensis MSMB43[1].

  • CAS Number: 1426953-24-3
  • MF: C30H46ClNO9
  • MW: 600.14
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1,2-Di-O-acetyl-3,5-di-O-benzyl-D-xylofuranose

1,2-Di-O-acetyl-3,5-di-O-benzyl-D-xylofuranose 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: 146986-45-0
  • MF: C23H26O7
  • MW: 414.45
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

B02

RAD51 Inhibitor B02 (B02) is an inhibitor of human RAD51 with an IC50 of 27.4 μM.

  • CAS Number: 1290541-46-6
  • MF: C22H17N3O
  • MW: 339.39000
  • Catalog: RAD51
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N6-iso-Propyladenosine

N6-iso-Propyladenosine 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: 17270-23-4
  • MF: C13H19N5O4
  • MW: 309.32
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A