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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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
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3'-Azido-3'-deoxy-5-Methyuridine

3’-Azido-3’-deoxy-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: 215176-58-2
  • MF: C10H13N5O5
  • MW: 283.24
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SRT3657

SRT3657 is a brain-permeable activator of SIRT1, with neuroprotective effect[1].

  • CAS Number: 1383551-17-4
  • MF: C40H54N8O6S
  • MW: 774.97
  • Catalog: Sirtuin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MPC 6827 hydrochloride

Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types[1][2].

  • CAS Number: 917369-31-4
  • MF: C17H18ClN3O
  • MW: 315.79700
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Amino-7-propargyl-7,8-dihydro-8-oxo-9-(beta-D-xylofuranosyl)purine

2-Amino-7-propargyl-7,8-dihydro-8-oxo-9-(beta-D-xylofuranosyl)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: 2389988-53-6
  • MF: C13H15N5O5
  • MW: 321.29
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SIRT5 inhibitor 4

SIRT5 inhibitor 4 (compound 11) is a potent, selective SIRT5 inhibitor with IC50 values of 26.4 and >400μM for SIRT5 and other SIRT subtype, respectively[1].

  • CAS Number: 708992-34-1
  • MF: C18H15N3O4S
  • MW: 369.39
  • Catalog: Sirtuin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ST247

ST247 a potent PPARβ/δ inverse agonist. ST247 has a higher affinity to PPARβ/δ. ST247 modulates expression of the activation marker CCL2 in the opposite direction. ST247 efficiently induces the interaction with corepressors. ST247 inhibits the agonist-induced transcriptional activity of PPARβ/δ[1].

  • CAS Number: 1356497-91-0
  • MF: C19H26N2O5S2
  • MW: 426.550
  • Catalog: PPAR
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 595.0±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 313.6±32.9 °C

Palmitic acid-d2-1

Palmitic acid-d2-1 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid 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: 62690-28-2
  • MF: C16H30D2O2
  • MW: 258.43600
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HDAC-IN-38

HDAC-IN-38 (compound 13) is a potent HDAC inhibitor. HDAC-IN-38 shows similar micro-molar inhibitory activity toward HDAC1, 2, 3, 5, 6, and 8. HDAC-IN-38 increases cerebral blood flow (CBF), attenuates cognitive impairment, and improves hippocampal atrophy. HDAC-IN-38 also increases the level of histone acetylation (H3K14 or H4K5)[1].

  • CAS Number: 2408123-36-2
  • MF: C27H28ClN3O2
  • MW: 461.98
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

6-Thio-2'-Deoxyguanosine

6-Thio-2'-Deoxyguanosine is a nucleoside analogue that can be incorporated into de novo-synthesized telomeres by telomerase.

  • CAS Number: 789-61-7
  • MF: C10H13N5O3S
  • MW: 283.307
  • Catalog: DNA/RNA Synthesis
  • Density: 2.0±0.1 g/cm3
  • Boiling Point: 709.1±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 382.6±35.7 °C

N4-Benzo yl-5’-O-(4,4’-dimethoxytrityl)-aracytidine

N4-Benzo yl-5’-O-(4,4’-dimethoxytrityl)-aracytidine 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: 87418-76-6
  • MF: C37H35N3O8
  • MW: 649.69
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SG2057

SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent[1].

  • CAS Number: 260417-62-7
  • MF: C33H36N4O6
  • MW: 584.662
  • Catalog: ADC Cytotoxin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 820.0±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 449.7±34.3 °C

N4-Bz-5'-O-DMTr-3'-deoxy-3'-fluoro-beta-D-xylofuranosyl cytidine-2'-CED-phosphoramidite

N4-Benzoyl-5’-O-(4,4’-dimethoxytrityl)-3’-deoxy-3’-fluoro-beta-D-xylofuranosyl cytidine-2’-CED-phosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.

  • CAS Number: 1555759-30-2
  • MF: C46H51FN5O8P
  • MW: 851.90
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Hydroxy-N'-(4-iodophenyl)octanediamide

4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC50s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) can be used for the research of cancer[1].

  • CAS Number: 1219807-87-0
  • MF: C14H19IN2O3
  • MW: 390.217
  • Catalog: HDAC
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Aldoxorubicin•HCl

Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.

  • CAS Number: 1361563-03-2
  • MF: C37H43ClN4O13
  • MW: 787.21
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-Deoxy-3’-α-C-methyl-5-methyluridine

3’-Deoxy-3’-α-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: 847650-50-4
  • MF: C11H16N2O5
  • MW: 256.26
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Prunasin

Prunasin is a inhibitor of DNA Polymerase β[1].

  • CAS Number: 99-18-3
  • MF: C14H17NO6
  • MW: 295.29
  • Catalog: DNA/RNA Synthesis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 527.0±50.0 °C at 760 mmHg
  • Melting Point: 138-148ºC
  • Flash Point: 272.5±30.1 °C

CCT244747

CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.

  • CAS Number: 1404095-34-6
  • MF: C20H24N8O2
  • MW: 408.45700
  • Catalog: Checkpoint Kinase (Chk)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N6-Ethyl-2’-O-methyladenosine

N6-Ethyl-2’-O-methyladenosine 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: 157309-11-0
  • MF: C13H19N5O4
  • MW: 309.32
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Topoisomerase I inhibitor 2

Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect[1].

  • CAS Number: 2588211-44-1
  • MF: C18H15NO3
  • MW: 293.32
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’-O-Me-2-thio-U-3’-phos phoramidite

2’-O-Me-2-thio-U-3’-phos phoramidite 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: 302918-84-9
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CDK7-IN-5

CDK7-IN-5 is a CDK7 inhibitor with an IC50 value <100 nM. CDK7-IN-5 has anticancer effects. (WO2015154022A1 (Compound 104))[1].

  • CAS Number: 1817006-50-0
  • MF: C34H45N9O2
  • MW: 611.78
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’,3’-Bis(O-t-butyldimethylsilyl)-2-thiouridine

2’,3’-Bis(O-t-butyldimethylsilyl)-2-thiouridine 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: 2305415-97-6
  • MF: C21H40N2O5SSi2
  • MW: 488.79
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ragaglitazar

Ragaglitazar is a PPARα and PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic.

  • CAS Number: 222834-30-2
  • MF: C25H25NO5
  • MW: 419.47000
  • Catalog: PPAR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AT13387

Onalespib (AT13387) is a potent inhibitor of Hsp90, with a Kd of 0.71 nM.

  • CAS Number: 912999-49-6
  • MF: C24H31N3O3
  • MW: 409.521
  • Catalog: HSP
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 605.7±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 320.1±31.5 °C

Guanine-13C,15N2

Guanine-13C,15N2 is the 13C and 15N labeled Guanine[1]. Guanine (2-Aminohypoxanthine) is one of the fundamental components of nucleic acids (DNA and RNA). Guanine is a purine derivative, consisting of a fused pyrimidine-imidazole ring system with conjugated double bonds.

  • CAS Number: 202407-12-3
  • MF: C413CH5N315N2O
  • MW: 154.11
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Adenosine-d2

Adenosine-d2 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physio

  • CAS Number: 82741-17-1
  • MF: C10H11D2N5O4
  • MW: 269.25
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Gatifloxacin sesquihydrate

Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml)[1]. Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis in vivo.

  • CAS Number: 180200-66-2
  • MF: C19H22FN3O4.3/2H2O
  • MW: 804.834
  • Catalog: Bacterial
  • Density: 1.386 g/cm3
  • Boiling Point: 607.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 321.4ºC

4-Phenylbutyric acid

Benzenebutyric acid is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.

  • CAS Number: 1821-12-1
  • MF: C10H12O2
  • MW: 164.201
  • Catalog: HDAC
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 290.7±9.0 °C at 760 mmHg
  • Melting Point: 49-52ºC
  • Flash Point: 187.9±13.9 °C

Corin

Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.

  • CAS Number: 1808113-09-8
  • MF: C26H28N4O2
  • MW: 428.53
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HBV-IN-21

HBV-IN-21 (Compound II-8b) is an HBV DNA replication inhibitor with an IC50 of 2.2 µM. HBV-IN-21 can interact HBV 4 capsid protein with good affinity (KD = 60.0 μM)[1].

  • CAS Number: 2460957-52-0
  • MF: C17H17FN4OS2
  • MW: 376.47
  • Catalog: HBV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A