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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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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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 >
PROTAC E3 Ligase Ligand-Linker Conjugate Ligand for E3 Ligase PROTAC Linker PROTAC-linker Conjugate for PAC
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
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Androgen Receptor Aromatase Estrogen Receptor/ERR Progesterone Receptor Thyroid Hormone Receptor Others

HDAC-IN-45

HDAC-IN-45 (Compound 14) is a small molecule HDAC inhibitor and has anticancer activity, also can forms a hydrogenbond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively[1].

  • CAS Number: 2421122-61-2
  • MF: C25H20ClFN8O
  • MW: 502.93
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AzddMeC

AzddMeC (CS-92) is an antiviral nucleoside analogue and a potent potent, selective and orally active HIV-1 reverse transcriptase and HIV-1 replication inhibitor. In HIV-1-infected human PBM cells and HIV-1-infected human macrophages, the EC50 values of AzddMeC are 9 nM and 6 nM, respectively[1][2].

  • CAS Number: 87190-79-2
  • MF: C10H14N6O3
  • MW: 266.257
  • Catalog: HIV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PARP1-IN-14

PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor, with an IC50 of 0.6 ± 0.1 nM. PARP1-IN-14 exhibits antiproliferative effect against both MDA-MB-436 (BRCA1−/−) and Capan-1 (BRCA2−/−) cells with IC50 values below 0.3 nM[1].

  • CAS Number: 2098639-70-2
  • MF: C28H24FN7O3
  • MW: 525.53
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’-dG (iBu)-2’-phosphoramidite

2’-dG (iBu)-2’-phosphoramidite 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: 157327-97-4
  • MF: C45H55N6O8P
  • MW: 838.93
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Topotecan hydrochloride hydrate

Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity[1].

  • CAS Number: 1044663-62-8
  • MF: C23H26ClN3O6
  • MW: 475.92
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Adenosine-2′-13C

Adenosine-2′-13C is the 13C 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 physiolo

  • CAS Number: 714950-52-4
  • MF: C10H13N5O4
  • MW: 268.23400
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-chloro-3'-deoxyadenosine

2-Chloro-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: 115044-75-2
  • MF: C10H12ClN5O3
  • MW: 285.69
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.03g/cm3
  • Boiling Point: 547.6ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 285ºC

((3aR,5R,6S,6aR)-6-Hydroxy-2,2-Dimethyltetrahydrofuro[2,3-D][1,3]Dioxol-5-Yl)Methyl 4-Methylbenzoate

1,2-Di-O-isopropylidene-5-O-(4-methylbenzoyl)-α-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: 75096-60-5
  • MF: C18H24O4
  • MW: 304.38
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Curvulin

Curvulin, isolated from Curvularia lunata, is a phytotoxin[1]. Curvularin is reported to inhibit microtubule assembly and has also been shown to inhibit iNOS expression.

  • CAS Number: 19054-27-4
  • MF: C12H14O5
  • MW: 238.23700
  • Catalog: Microtubule/Tubulin
  • Density: 1.273g/cm3
  • Boiling Point: 404.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 155.3ºC

Proscillaridin A

Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively[1].

  • CAS Number: 466-06-8
  • MF: C30H42O8
  • MW: 530.650
  • Catalog: Topoisomerase
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 716.7±60.0 °C at 760 mmHg
  • Melting Point: 233ºC
  • Flash Point: 232.6±26.4 °C

Naringenin

Naringenin is the predominant flavanone in grapefruit; displays strong anti-inflammatory and antioxidant activities.

  • CAS Number: 480-41-1
  • MF: C15H12O5
  • MW: 272.253
  • Catalog: Influenza Virus
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 577.5±50.0 °C at 760 mmHg
  • Melting Point: 247-250 °C(lit.)
  • Flash Point: 224.7±23.6 °C

RKI-1313

RKI-1313 is a ROCK inhibitor with IC50s of 34, 8 µM for ROCK 1 and ROCK 2, respectively. RKI-1313 shows little effect on the phosphorylation levels of ROCK substrates, migration, invasion or anchorage-independent growth[1].

  • CAS Number: 1342276-76-9
  • MF: C17H16N4O2S
  • MW: 340.400
  • Catalog: ROCK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pemetrexed disodium hydrate

Pemetrexed disodium hemipenta hydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.

  • CAS Number: 357166-30-4
  • MF: C20H21N5O6.5/2H2O.2Na
  • MW: 516.41
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DOLASTATIN 10

Dolastatin 10 is a potent antimitotic peptide, isolated from the marine mollusk Dolabela auricularia, that inhibits tubulin polymerization.

  • CAS Number: 110417-88-4
  • MF: C42H68N6O6S
  • MW: 785.091
  • Catalog: Peptides
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 903.6±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 500.3±34.3 °C

2-Amino-9-((2S,4R,5S)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-3H-purin-6(9H)-one

2'-Deoxy-L-guanosine selectively inhibits D-Thymidine phosphorylation catalyzed by HSV 1 thymidine kinase.2'-Deoxy-L-guanosine is the L-configuration of 2'-Deoxyguanosine (HY-17563)[1].

  • CAS Number: 22837-44-1
  • MF: C11H14N4O4
  • MW: 266.25300
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’,5’-Di-O-acetyl-2’-deoxy-N3-methyl uridine

3’,5’-Di-O-acetyl-2’-deoxy-N3-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: 2305416-14-0
  • MF: C14H18N2O7
  • MW: 326.30
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3'-Deoxyinosine

3'-Deoxyinosine 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: 13146-72-0
  • MF: C10H12N4O4
  • MW: 252.23
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.9±0.1 g/cm3
  • Boiling Point: 681.2±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 365.8±34.3 °C

Ethylenediaminetetraacetic acid dipotassium salt dihydrate

Ethylenediaminetetraacetic acid (EDTA) dipotassium dihydrate is anticoagulants, chelating heavy metal and relieve toxicity. Ethylenediaminetetraacetic acid dipotassium dihydrate can damage chromosomes, interfere with the DNA repair process, increase the incidence of meiosis exchange[1].

  • CAS Number: 25102-12-9
  • MF: C10H18K2N2O10
  • MW: 404.45
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: 614.2ºC at 760 mmHg
  • Melting Point: 255-280 °C (dec.)(lit.)
  • Flash Point: 325.2ºC

5-(Furan-2-yl)-2’-O-methyl-5’-O-DMTr-cytidine

5-(Furan-2-yl)-2’-O-methyl-5’-O-DMTr-cytidine 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: 2095417-02-8
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-AMINO-6-CHLORO-9-(3,5-DI-O-(P-TOLUOYL)-BETA-D-2-DEOXYRIBOFURNANOSYL)PURINE

2-Amino-6-chloropurine-9-beta-D-(2’-deoxy-3’,5’-di-O-(p-toluoyl))riboside 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: 35095-93-3
  • MF: C26H24ClN5O5
  • MW: 521.95
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5’(R)-C-Methyl-2-thiouridine

5’(R)-C-Methyl-2-thiouridine 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: 2305416-01-5
  • MF: C10H14N2O5S
  • MW: 274.29
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

A09-003

A09-003 is a CDK-9 inhibitor (IC50: 16 nM). A09-003 inhibits leukemia cell proliferation (IC50: 1.90, 0.86, 2.49, 1.84, 0.48 μM for BDCM, Molm-14, THP-1, U937, MV4-11 cells). A09-003 induces apoptosis and decreases Mcl-1 expression through Thr163 dephosphorylation[1].

  • CAS Number: 2911646-14-3
  • MF: C23H26N4O
  • MW: 374.48
  • Catalog: Bcl-2 Family
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-Deoxy-3’-fluoro-5-methylcytidine

3’-Deoxy-3’-fluoro-5-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: 847650-07-1
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Epothilone F

Epothilone F is a Microtubule/Tubulin-stabilizing agent with anti-tumor activity. Epothilone F inhibits the proliferation of breast cancer cells, non-small cell lung cancer cells, drug-resistant ovarian cancer cells[1].

  • CAS Number: 208518-52-9
  • MF: C27H41NO7S
  • MW: 523.68200
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3'-Deoxy-5-methyluridine

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: 7084-29-9
  • MF: C10H14N2O5
  • MW: 242.23
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 530.01 °C(Predicted)
  • Melting Point: 226.62 °C
  • Flash Point: N/A

Adenosine, 4'-thio-

4’-Thioadenosine 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: 2500-80-3
  • MF: C10H13N5O3S
  • MW: 283.31
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.08g/cm3
  • Boiling Point: 657.8ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 351.6ºC

L82

L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM). L82 shows anti-proliferative activity to breast cancer cells[1][2].

  • CAS Number: 329227-30-7
  • MF: C11H8ClN5O4
  • MW: 309.67
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N4-Benzoyl-7'-OH-N-trityl Morpholino cytosine

N4-Benzoyl-7’-OH-N-trityl morpholino cytosine 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: 125515-31-3
  • MF: C35H32N4O4
  • MW: 572.65
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Saccharin 1-methylimidazole

Saccharin 1-methylimidazole is an activator for DNA/RNA Synthesis.

  • CAS Number: 482333-74-4
  • MF: C11H11N3O3S
  • MW: 265.29
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1,N6-Ethenoadenosine

1,N6-Ethenoadenosine 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: 39007-51-7
  • MF: C12H13N5O4
  • MW: 291.26
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.99g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A