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 >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
Apoptosis >
Apoptosis Bcl-2 Family c-Myc Caspase DAPK Ferroptosis IAP MDM-2/p53 PKD RIP kinase Survivin Thymidylate Synthase TNF Receptor
Autophagy >
Autophagy LRRK2 ULK Mitophagy
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Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
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Arp2/3 Complex Dynamin Gap Junction Protein Integrin Kinesin Microtubule/Tubulin Mps1 Myosin PAK
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Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
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Vitamin D Related >
VD/VDR
Others >
Androgen Receptor Aromatase Estrogen Receptor/ERR Progesterone Receptor Thyroid Hormone Receptor Others

Mafosfamide Sodium Salt

Mafosfamide sodium salt (Z 7557 sodium salt) targets nuclear DNA, forms DNA cross-links and inhibits DNA synthesis. Mafosfamide sodium salt, a cyclophosphamide analogue, induces apoptosis in lymphoblastoid cells. Mafosfamide sodium salt has antitumor activity[1][2].

  • CAS Number: 84211-05-2
  • MF: C9H18Cl2N2NaO5PS2
  • MW: 401.26700
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ac-Glu-Ser-Met-Asp-aldehyde (pseudo acid)

Ac-ESMD-CHO is an inhibitor of caspase-3 and caspase-7. Ac-ESMD-CHO inhibits proteolytic cleavage of the caspase-3 precursor peptide (CPP32) at the Glu-Ser-Met-Asp (ESMD) site[1][2].

  • CAS Number: 191338-87-1
  • MF: C19H30N4O10S
  • MW: 506.527
  • Catalog: Casein Kinase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 1049.7±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 588.6±34.3 °C

Crolibulin

Crolibulin is a small molecule tubulin polymerization inhibitor.

  • CAS Number: 1000852-17-4
  • MF: C18H17BrN4O3
  • MW: 417.25700
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JPS035

JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells[1].

  • CAS Number: 2669785-84-4
  • MF: C49H65N7O7S
  • MW: 896.15
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’,5’-Di-O-benzoyl-2’-deoxy-2’-fluoro-5-methyl-β-D-arabino-uridine

3’,5’-Di-O-benzoyl-2’-deoxy-2’-fluoro-5-methyl-β-D-arabino-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: 97614-47-6
  • MF: C24H21FN2O7
  • MW: 468.43
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BMS-3

BMS-3 is a potent LIMK inhibitor with IC50s of 5 nM and 6 nM for LIMK1 and LIMK2, respectively.

  • CAS Number: 1338247-30-5
  • MF: C17H12Cl2F2N4OS
  • MW: 429.271
  • Catalog: LIM Kinase (LIMK)
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5,10,15,20-Tetrakis(N-methyl-4-pyridyl)porphine tetratosylate

TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1[1]. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines[2].

  • CAS Number: 36951-72-1
  • MF: C72H66N8O12S4
  • MW: 1363.60
  • Catalog: G-quadruplex
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GeA-69

GeA-69 is a selective, highly cell permeable allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2, with a Kd of 2.1 µM[1].

  • CAS Number: 2143475-98-1
  • MF: C20H16N2O
  • MW: 300.35
  • Catalog: PARP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Myoseverin

Myoseverina, a microtubule-binding molecule, induces the reversible fission of multinucleated myotubes into mononucleated fragments. Myoseverina affects the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with the activation of pathways involved in wound healing and tissue regeneration[1].

  • CAS Number: 267402-71-1
  • MF: C24H28N6O2
  • MW: 432.518
  • Catalog: Microtubule/Tubulin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 661.3±65.0 °C at 760 mmHg
  • Melting Point: 108 °C
  • Flash Point: 353.7±34.3 °C

AVG-233

AVG-233 (AVG233) is a potent, allosteric inhibitor of respiratory syncytial virus (RSV) RNA-dependent RNA polymerase (RdRp) complex, demonstrates nanomolar activity against both laboratory-adapted RSV strains and clinical RSV isolates (EC50=34-79 nM); exhibits 34% oral bioavailability and sustained high drug levels in the circulation after a single oral dose of 20 mg/kg.

  • CAS Number: 2151937-80-1
  • MF: C26H22ClN5O3
  • MW: 487.944
  • Catalog: RSV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Phleomycin

Phleomycin is a wide-spectrum glycopeptide antibiotic found in Streptomyces verticillus. Phleomycin, an effective DNA-cleaving agent, binds and intercalates DNA to damage the integrity of the double helix, which is similar to Bleomycin (HY-17565A)[1].

  • CAS Number: 11006-33-0
  • MF: C52H75N16O21S2
  • MW: 1324.38000
  • Catalog: Bacterial
  • Density: 1.83 g/cm3
  • Boiling Point: 1718.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 993.3ºC

DETIVICICLOVIR

Detiviciclovir (AM365) is an antiviral nucleoside analogue[1].

  • CAS Number: 220984-26-9
  • MF: C9H13N5O2
  • MW: 223.23200
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.63g/cm3
  • Boiling Point: 603.2ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 318.6ºC

Fanotaprim

Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis[1].

  • CAS Number: 2120282-75-7
  • MF: C19H22N8O
  • MW: 378.43
  • Catalog: Antifolate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Podophyllotoxinone

Podophyllotoxone is isolated from the roots of Dysosma versipellis and has anti-cancer activities.Podophyllotoxone is able to inhibit the tubulin polymerization[1].

  • CAS Number: 477-49-6
  • MF: C22H20O8
  • MW: 412.38900
  • Catalog: Microtubule/Tubulin
  • Density: 1.365 g/cm3
  • Boiling Point: 602.3±55.0℃ at 760 mmHg
  • Melting Point: 191.73℃
  • Flash Point: N/A

Thymidine, a-azido- (9CI)

α-Azidothymidine 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: 59090-48-1
  • MF: C10H13N5O5
  • MW: 283.24
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HDAC-IN-28

HDAC-IN-28, a novel HDAC inhibitor, shows potent activities against tumor growth and metastasis

  • CAS Number: 1621154-88-8
  • MF: C23H26N4O4S
  • MW: 454.54
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Neocarzinostatin

Neocarzinostatin, a potent DNA-damaging, anti-tumor antibiotic, recognizes double-stranded DNA bulge and induces DNA double strand breaks (DSBs). Neocarzinostatin induces apoptosis. Neocarzinostatin has potential for EpCAM-positive cancers treatment [1][2].

  • CAS Number: 9014-02-2
  • MF: C35H35NO12
  • MW: 661.65200
  • Catalog: Apoptosis
  • Density: 1.52g/cm3
  • Boiling Point: 900.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 498.4ºC

Aminohexylgeldanamycin

Aminohexylgeldanamycin (AHGDM), a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin shows antiangiogenic and antitumor activities[1].

  • CAS Number: 485395-71-9
  • MF: C34H52N4O8
  • MW: 644.80
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rev 2’-O-MOE-5MeU-5’-amidite

Rev 2’-O-MOE-5MeU-5’-amidite 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: 1345715-43-6
  • MF: C43H55N4O10P
  • MW: 818.89
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-Methyl-2'-C-methyluridine

2’-β-C-Methyl-5-methyluridine 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: 119410-84-3
  • MF: C11H16N2O6
  • MW: 272.25
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Eg5 Inhibitor V, trans-24

Eg5 Inhibitor V, trans-24 is a potent and specific Eg5 inhibitor with an IC50 of 0.65 μM, and can be used in the research of cancer.

  • CAS Number: 869304-55-2
  • MF: C26H21N3O3
  • MW: 423.46300
  • Catalog: Kinesin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thiomyristoyl

Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM.

  • CAS Number: 1429749-41-6
  • MF: C34H51N3O3S
  • MW: 581.8612
  • Catalog: Sirtuin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Patritumab

Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and Akt. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors[1].

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

K00546

K00546 is a potent inhibitor of the CDC2-like kinase CLK1 and CLK3 with IC50 of 8.9 and 29.2 nM, respectively.

  • CAS Number: 443798-47-8
  • MF: C15H13F2N7O2S2
  • MW: 425.436
  • Catalog: CDK
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: 649.1±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 346.4±34.3 °C

5'-O-DMTr-3'-O-methyl uridine-3'-CED-phosphoramidite

5'-O-DMTr-3'-O-methyl uridine-3'-CED-phosphoramidite 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: 179479-05-1
  • MF: C40H49N4O9P
  • MW: 760.8
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ZINC194100678

ZINC194100678 is a potent PAK1 inhibitor with an IC50 value of 8.37 μM. ZINC194100678 can inhibit MDA-MB-231 cell proliferation. ZINC194100678 can be used for researching anticancer[1].

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

CG347B

CG347B is a selective HDAC6 inhibitor[1].

  • CAS Number: 1598426-03-9
  • MF: C16H17N3O2
  • MW: 283.325
  • Catalog: HDAC
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 457.2±47.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 230.3±29.3 °C

Flurocitabine

Flurocitabine is a fluorinated anlydride analog of cytosine arabinoside, partially hydrolysecl in vivo into two active antitumor substances (arabinosyl-tluorocytosine (ara-FC) and arabinosyl-fluorouracil (ara-FU)). Flurocitabine has antitumor activity during phase I studies in acute leukemia and solid tumors[1].

  • CAS Number: 37717-21-8
  • MF: C9H10FN3O4
  • MW: 243.19200
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.11g/cm3
  • Boiling Point: 391.7ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 190.7ºC

m7GpppUmpG

m7GpppUmpG, an oligonucleotide, is an M7GpppNpG trinucleotide cap analogue. m7GpppUmpG can be used as a chemical tool enabling manufacturing of RNA featuring either cap 0 or cap 1 structures[1].

  • CAS Number: 2638447-87-5
  • MF: C31H42N12O26P4
  • MW: 1122.63
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bz-rA Phosphoramidite

Bz-rA Phosphoramidite is used for ribonucleotides modification[1].

  • CAS Number: 104992-55-4
  • MF: C53H66N7O8PSi
  • MW: 988.193
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A