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
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 >
AMPK Aurora Kinase DNA Methyltransferase Epigenetic Reader Domain HDAC Histone Acetyltransferase Histone Demethylase Histone Methyltransferase JAK MicroRNA PARP PKC Sirtuin Protein Arginine Deiminase
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Immunology/Inflammation >
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JAK/STAT Signaling >
EGFR JAK Pim STAT
MAPK/ERK Pathway >
ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel >
ATP Synthase BCRP Calcium Channel CFTR Chloride Channel CRAC Channel CRM1 EAAT2 GABA Receptor GlyT HCN Channel iGluR Monoamine Transporter Monocarboxylate Transporter Na+/Ca2+ Exchanger Na+/HCO3- Cotransporter Na+/K+ ATPase nAChR NKCC P-glycoprotein P2X Receptor Potassium Channel Proton Pump SGLT Sodium Channel TRP Channel URAT1
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
Stem Cell/Wnt >
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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TGF-beta/Smad PKC ROCK TGF-β Receptor
Vitamin D Related >
VD/VDR
Others >
Androgen Receptor Aromatase Estrogen Receptor/ERR Progesterone Receptor Thyroid Hormone Receptor Others

SCR7

SCR7 is a DNA Ligase IV inhibitor with anticancer activity.

  • CAS Number: 1533426-72-0
  • MF: C18H14N4OS
  • MW: 334.395
  • Catalog: CRISPR/Cas9
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 644.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 343.8±34.3 °C

Phenylacetic acid mustard

Phenylacetic acid mustard is the major metabolite of the cancer chemotherapeutic agent Chlorambucil (HY-13593). Chlorambucil is an alkylating agent with antitumor activity[1].

  • CAS Number: 10477-72-2
  • MF: C12H15Cl2NO2
  • MW: 276.15900
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: 195.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 89.6ºC

Palmitic acid-13C sodium

Palmitic acid-13C sodium is the 13C-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: 201612-54-6
  • MF: C1513CH31NaO2
  • MW: 279.40
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SCR7 pyrazine

SCR7 pyrazine is a DNA ligase IV inhibitor that blocks nonhomologous end-joining (NHEJ) in a ligase IV-dependent manner. SCR7 pyrazine is also a CRISPR/Cas9 enhancer which increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cell apoptosis and has anticancer activity[1][2].

  • CAS Number: 14892-97-8
  • MF: C18H12N4OS
  • MW: 332.37900
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 209 °C
  • Flash Point: N/A

Gsk317354a

GSK317354A is a ROCK and GRK inhibitor. GSK317354A can be used for heart failure and Parkinson’s disease research[1].

  • CAS Number: 874119-13-8
  • MF: C25H18F4N6O
  • MW: 494.44
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

depudecin

Depudecin ((-)-Depudecin) is a histone deacetylase (HDAC) inhibitor. Depudecin can be isolated from the fungus Alternaria brassicicola[1][2].

  • CAS Number: 139508-73-9
  • MF: C11H16O4
  • MW: 212.24200
  • Catalog: HDAC
  • Density: 1.415g/cm3
  • Boiling Point: 369.4ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 177.2ºC

USP7-IN-10

USP7-IN-10 (compound 1) is a potent ubiquitin-specific protease 7 (USP7) inhibitor, with an IC50 of 13.39 nM[1].

  • CAS Number: 2755995-01-6
  • MF: C26H29ClN4O3S
  • MW: 513.05
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin polymerization-IN-11

Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 µM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP[1].

  • CAS Number: 2470063-59-1
  • MF: C22H22N4O4
  • MW: 406.43
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3'-(O-METHYL)INOSINE

3’-O-Methyl inosine 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: 75479-64-0
  • MF: C11H14N4O5
  • MW: 282.25
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4-AMINO-1,8-NAPHTHALIMIDE

4-Aminonaphthalimide is a potent PARP inhibitor and potentiates the cytotoxicity of γ-radiation in cancer cells[1].

  • CAS Number: 1742-95-6
  • MF: C12H8N2O2
  • MW: 212.20
  • Catalog: PARP
  • Density: 1.105 g/mL at 25ºC(lit.)
  • Boiling Point: 544.1ºC at 760 mmHg
  • Melting Point: 360ºC
  • Flash Point: 282.8ºC

CDK7-IN-16

CDK7-IN-16 (compound 9) is a potent CDK 7 inhibitor with an IC50 range of 1 ~ 10 nM. CDK7-IN-16 can be used for researching anticancer, especially the cancer with transcriptional dysregulation[1].

  • CAS Number: 2765676-32-0
  • MF: C19H21F3N6O2S
  • MW: 454.47
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2'-DEOXYGUANOSINE 5'-TRIPHOSPHATE DILITHIUM SALT

dGTP-15N5 (2'-Deoxyguanosine-5'-triphosphate-15N5) dilithium is 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.

  • CAS Number: 95648-75-2
  • MF: C10H14Li2N5O13P3
  • MW: 519.04700
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin polymerization-IN-13

Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity[1].

  • CAS Number: 2426665-56-5
  • MF: C20H21NO6
  • MW: 371.38
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

6-mercaptopurine-2'-deoxyriboside

2′-Deoxy-6-thioinosine 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: 2239-64-7
  • MF: C10H12N4O3S
  • MW: 268.29
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.87g/cm3
  • Boiling Point: 665.9ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 356.5ºC

Tankyrase-IN-3

Tankyrase-IN-3 is a tankyrase 1 (TNKS1) inhibitor with an IC50 value of 22 nM. Tankyrase-IN-3 can be used for the research of cancer[1].

  • CAS Number: 938893-79-9
  • MF: C21H21N5O4
  • MW: 407.42
  • Catalog: PARP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fialuridine

Fialuridine is a nucleoside analog with antiviral activity[1].

  • CAS Number: 69123-98-4
  • MF: C9H10FIN2O5
  • MW: 372.09
  • Catalog: DNA/RNA Synthesis
  • Density: 2.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 216-217ºC
  • Flash Point: N/A

4′,5′-Didehydro-2′,5′-dideoxyuridine

4′,5′-Didehydro-2′,5′-dideoxyuridine 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: 58096-66-5
  • MF: C9H10N2O4
  • MW: 210.19
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PF-670462

PF-670462 is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.

  • CAS Number: 950912-80-8
  • MF: C19H22Cl2FN5
  • MW: 410.316
  • Catalog: Casein Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m7GpppUpG

m7GpppUpG, an oligonucleotide, is an M7GpppNpG trinucleotide cap analogue. m7GpppUpG can be used as a chemical tool enabling manufacturing of RNA featuring either cap 0 or cap 1 structures[1].

  • CAS Number: 2638447-85-3
  • MF: C30H40N12O26P4
  • MW: 1108.60
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CL-216942

Bisantrene dihydrochloride is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene dihydrochloride targets eukaryotic type II topoisomerases. Bisantrene dihydrochloride is a substrate of MDR1[1][2][3][4].

  • CAS Number: 71439-68-4
  • MF: C22H23ClN8
  • MW: 434.92500
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: 646.3ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 344.7ºC

N6-Benzoyl-5'-O-DMT-3'-O-methyladenosine 3'CE-phosphoramidite

N6-Benzoyl-5'-O-DMT-3'-O-methyladenosine 3'CE-phosphoramidite 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: 179479-02-8
  • MF: C48H54N7O8P
  • MW: 887.96
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ciglitazone

Ciglitazone is a potent and selective PPARγ agonist (EC50=3 μM). Ciglitazone inhibits proliferation and differentiation of th17 cells. Ciglitazone is a hypoglycemic agent orally active in the obese-hyperglycemic animal models. Ciglitazone induces apoptosis accompanied by activation of p38 MAPK and nuclear translocation of apoptosis inducing factor (AIF) in opossum kidney (OK) renal epithelial cells[1][2][3][4].

  • CAS Number: 74772-77-3
  • MF: C18H23NO3S
  • MW: 333.445
  • Catalog: PPAR
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 504.5±23.0 °C at 760 mmHg
  • Melting Point: 130-131ºC
  • Flash Point: 258.9±22.6 °C

script

Nullscript is a negative control for Scriptaid. Nullscript is a known inactive analog of Scriptaid[1]. Scriptaid is a representative HDAC inhibitor[2]. Nullscript inhibits Cryptosporidium (C. parvum) growth with the IC50 value of 2.1 μM[3].

  • CAS Number: 300816-11-9
  • MF: C16H14N2O4
  • MW: 298.293
  • Catalog: HDAC
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CMC·HCI

5-Methylcyclocytidine hydrochloride 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: 51391-96-9
  • MF: C10H14ClN3O4
  • MW: 275.69
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Microtubule inhibitor 1

Microtubule inhibitor 1 is an antitumor agent with microtubule polymerization inhibitory activity, with an IC50 value of 9-16 nM in cancer cells[1].

  • CAS Number: 2305668-80-6
  • MF: C21H19NO3
  • MW: 333.38
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2'-Deoxy-N4-methylcytidine

2’-Deoxy-N4-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: 22882-02-6
  • MF: C10H15N3O4
  • MW: 241.24
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.56g/cm3
  • Boiling Point: 460.5ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 232.3ºC

PluriSIn #2

PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). PluriSIn #2 is a compound that selectively eliminates undifferentiated human pluripotent stem cells (hPSCs)[1].

  • CAS Number: 56563-17-8
  • MF: C11H8FN3O3
  • MW: 249.19800
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5'-O-DMT-N4-Benzoyl-5-methyl-2'-O-methylcytidine 3'-CE phosphoramidite

5-Me-DMT-2'-O-Me-C(Bz)-CE-Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.

  • CAS Number: 166593-57-3
  • MF: C48H56N5O9P
  • MW: 877.96
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ATR-IN-10

ATR-IN-10 is a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase with an IC50 value of 2.978 μM.

  • CAS Number: 2713577-93-4
  • MF: C27H24N4O
  • MW: 420.51
  • Catalog: ATM/ATR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3'-O-tert-Butyldimethylsilyl-5'-O-DMT-2'-deoxyadenosine

3'-O-tert-Butyldimethylsilyl-5'-O-DMT-2'-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: 89947-86-4
  • MF: C37H45N5O5Si
  • MW: 667.87
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A