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 >
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Cell Cycle/DNA Damage >
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
Cytoskeleton >
Arp2/3 Complex Dynamin Gap Junction Protein Integrin Kinesin Microtubule/Tubulin Mps1 Myosin PAK
Epigenetics >
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JAK/STAT Signaling >
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ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel >
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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 >
NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
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Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
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Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
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Vitamin D Related >
VD/VDR
Others >
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Malonganenone A

Malonganenone A is a selective plasmodial Hsp70s modulator. It also has antimalarial activity.

  • CAS Number: 882403-69-2
  • MF: C26H38N4O2
  • MW: 438.61
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-Deoxy-3’-fluoro-xylocytidine

3’-Deoxy-3’-fluoro-xylocytidine 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: 26563-01-9
  • MF: C9H12FN3O4
  • MW: 245.21
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.8±0.1 g/cm3
  • Boiling Point: 500.1±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 256.2±32.9 °C

KW-2478

KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.

  • CAS Number: 819812-04-9
  • MF: C30H42N2O9
  • MW: 574.662
  • Catalog: HSP
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 746.9±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 405.5±32.9 °C

Mertansine

Mertansine (DM1) is a microtubulin inhibitor which binds at the tips of microtubules and suppresses the dynamicity of microtubules.. Mertansine is an antibody-conjugatable maytansinoid that was developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.

  • CAS Number: 139504-50-0
  • MF: C35H48ClN3O10S
  • MW: 738.288
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: 1.33±0.1 g/cm3
  • Boiling Point: 937.1±65.0 °C at 760 mmHg
  • Melting Point: 190-192 ºC
  • Flash Point: 520.5±34.3 °C

Uridine 13C

Uridine 13C is the 13C labeled Uridine[1].

  • CAS Number: 201996-62-5
  • MF: C9H12N2O6
  • MW: 245.19400
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Daunorubicin HCl

Daunorubicin hydrochloride is a topoisomerase II inhibitor with potent antineoplastic activities.

  • CAS Number: 23541-50-6
  • MF: C27H30ClNO10
  • MW: 563.981
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: 770ºC at 760 mmHg
  • Melting Point: 188 - 190ºC
  • Flash Point: 419.5ºC

2’-Deoxy-2’-fluoro-5-methyl-4’-thio-a-D-arabino uridine

2’-Deoxy-2’-fluoro-5-methyl-4’-thio-a-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: 294868-24-9
  • MF: C10H13FN2O4S
  • MW: 276.28
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N6-BENZOYL-5'-O-(DIMETHOXYTRITYL)-3'-DEOXYADENOSINE

N-Benzoyl-5′-O-[bis(4-methoxyphenyl)phenylmethyl]-3′-deoxyadenosine 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: 84138-86-3
  • MF: C38H35N5O6
  • MW: 657.71
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Adenosine,2'-chloro-2'-deoxy-

2’-Chloro-2’-deoxyadenosine 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: 2627-62-5
  • MF: C10H12ClN5O3
  • MW: 285.69
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.03g/cm3
  • Boiling Point: 678.2ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 364ºC

Apcin

Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis[1][2][3].

  • CAS Number: 300815-04-7
  • MF: C13H14Cl3N7O4
  • MW: 438.65400
  • Catalog: APC
  • Density: 1.68±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine

3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine (Compound 7) is an inhibitor of protein kinases, with IC50s of 0.092, 0.26, 0.77 μM for PKC-α, ROCK, ASK1. 3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine shows potent cytotoxicity against PC-3 cancer cells with an IC50 value of 0.16 μM[1].

  • CAS Number: 2226941-29-1
  • MF: C28H24N4O4
  • MW: 480.51
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Phen-DC 3

Phen-DC3 is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases with IC50s of 65±6 and 50±10 nM, respectively.

  • CAS Number: 942936-75-6
  • MF: C34H26N6O2
  • MW: 550.61
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cyclophosphamide (hydrate)

Cyclophosphamide hydrate is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic and immunosuppressive activities.

  • CAS Number: 6055-19-2
  • MF: C7H17Cl2N2O3P
  • MW: 279.101
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: 336.1ºC at 760 mmHg
  • Melting Point: 49-51 °C(lit.)
  • Flash Point: >230 °F

2’-Deoxy-3’,2-anhydrouridine

2’-Deoxy-3’,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: 26922-44-1
  • MF: C9H10N2O4
  • MW: 210.19
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Palmitic acid-13C16 sodium

Palmitic acid-13C16 sodium is the 13C-labeled Palmitic acid sodium. Palmitic acid sodium is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid sodium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].

  • CAS Number: 2483736-17-8
  • MF: 13C16H31NaO2
  • MW: 294.29
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2′-Deoxy-β-L-uridine

2'-Deoxy-β-L-uridine is a nucledside analogue and a specific substrate for the viral enzyme, shows no stereospecificity against herpes simplex 1 (HSV1) thymidine kinase (TK). 2′-Deoxy-β-L-uridine exerts antiviral activity via the interation of 5'-triphosphates with the viral DNA polymerase[1][2].

  • CAS Number: 31501-19-6
  • MF: C9H11N2O5+
  • MW: 227.19400
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.533 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

cyclothialidine

Cyclothialidine ( Ro 09-1437) is a potent DNA gyrase inhibitor isolated from Streptomyces filipinensisNR0484[1].

  • CAS Number: 147214-63-9
  • MF: C26H35N5O12S
  • MW: 641.64700
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-Amino-3’-deoxy-5-fluorouridine

3’-Amino-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: 80955-97-1
  • MF: C9H12FN3O5
  • MW: 261.21
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Deoxy-2’-deoxy-5’-(4,4’-dimethoxytrityl)uridine

2-Deoxy-2’-deoxy-5’-(4,4’-dimethoxytrityl)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: 151503-26-3
  • MF: C30H30N2O6
  • MW: 514.57
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’,3’-Di-O-acetyl-8-benzyloxy-3’-deoxy guanosine

2’,3’-Di-O-acetyl-8-benzyloxy-3’-deoxy guanosine 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: 2389988-71-8
  • MF: C21H23N5O7
  • MW: 457.44
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ryuvidine

Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC50 of 0.5 µM and suppresses monomethylation of H4K20 in vitro[1]. Ryuvidine also inhibits CDK4 with an IC50 of 6.0 μM and is cytotoxic against a range of human cancer cells[2].

  • CAS Number: 265312-55-8
  • MF: C15H12N2O2S
  • MW: 284.33300
  • Catalog: CDK
  • Density: 1.416g/cm3
  • Boiling Point: 463.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 234.3ºC

HDACs/mTOR Inhibitor 1

HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis with low toxicity in vivo[1].

  • CAS Number: 2271413-06-8
  • MF: C28H38N8O5
  • MW: 566.65
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

11α-O-Tigloyl-12β-O-acetyltenacigenin B

11α-O-Tigloyl-12β-O-acetyltenacigenin B is an ester derivative of Tenacigenin B (HY-N1168), which is isolated from Garcinia cambogia (MTC). Tenacigenin B modulates the antitumor effects of Aurora-A in lymphoma.

  • CAS Number: 154022-51-2
  • MF: C28H40O7
  • MW: 488.61
  • Catalog: Aurora Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sirt1/2-IN-1

Sirt1/2-IN-1 (Compound 7) is a SIRT1 and SIRT2 inhibitor with IC50 values of 1.81, 2.10 and 20.5 µg/mL against SIRT1, SIRT2 and SIRT3, respectively. Sirt1/2-IN-1 displays activity in hyperacetylation of α-tubulin protein with an IC50 of 32.05 µg/mL. Sirt1/2-IN-1 shows prominent anticancer activity[1].

  • CAS Number: 2402779-21-7
  • MF: C22H13ClN2OS2
  • MW: 420.93
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ixabepilone

Ixabepilone is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.

  • CAS Number: 219989-84-1
  • MF: C27H42N2O5S
  • MW: 506.698
  • Catalog: Microtubule/Tubulin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 697.8±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 375.8±31.5 °C

N6-Benzoyl-2'-deoxy-5'-O-DMT-a-adenosine 3'-CE phosphoramidite

N6-Benzoyl-2'-deoxy-5'-O-DMT-a-adenosine 3'-CE phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.

  • CAS Number: 152695-84-6
  • MF: C47H52N7O7P
  • MW: 857.93
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Casein kinase 1δ-IN-10

Casein kinase 1δ-IN-10 is a casein kinase 1δ (CK1δ) inhibitor (WO2012080729A2; compound 685)[1].

  • CAS Number: 332074-85-8
  • MF: C21H17N3O3
  • MW: 359.38
  • Catalog: Casein Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Entasobulin

Entasobulin is a β-tubulin polymerization inhibitor with potential anticancer activity.

  • CAS Number: 501921-61-5
  • MF: C26H18ClN3O2
  • MW: 439.893
  • Catalog: Microtubule/Tubulin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cantuzumab mertansine

Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1; HY-19792) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts[1][2].

  • CAS Number: 400010-39-1
  • MF:
  • MW:
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’-Deoxy-2’-fluoro-alpha-D-arabinoguanosine

2’-Deoxy-2’-fluoro-alpha-D-arabinoguanosine 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: 2072145-29-8
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A