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 >
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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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8-Bromo-2'-deoxyadenosine

8-Bromo-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: 14985-44-5
  • MF: C10H12BrN5O3
  • MW: 330.14
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.3g/cm3
  • Boiling Point: 671ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 359.6ºC

2-Amino-6-chloropurine-9-beta-D-(2'-deoxy-3',5'-di-O-benzoyl-2'-fluoro)arabinoriboside

2-Amino-6-chloropurine -9-beta-D-(2’-deoxy-3’,5’-di-O-benzoyl-2’-fluoro)arabinoriboside 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: 118373-61-8
  • MF: C24H19ClFN5O5
  • MW: 511.89
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VXc-486

VXc-486 is a gyrase B inhibitor, with bactericidal activity. VXc-486 potently inhibits multiple drug-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively[1].

  • CAS Number: 1384984-18-2
  • MF: C21H25FN6O3
  • MW: 428.460
  • Catalog: Bacterial
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

scopolin

Scopolin is a coumarin isolated from Arabidopsis thaliana (Arabidopsis) roots[1]. Scopolin attenuated hepatic steatosis through activation of SIRT1-mediated signaling cascades[2].

  • CAS Number: 531-44-2
  • MF: C16H18O9
  • MW: 354.309
  • Catalog: Sirtuin
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 650.2±55.0 °C at 760 mmHg
  • Melting Point: 217ºC
  • Flash Point: 241.5±25.0 °C

3'-Adenylic acid

Adenosine 3′-monophosphate (3′-AMP), a nucleotide, is a cyclic AMP production agonist[1].

  • CAS Number: 84-21-9
  • MF: C10H14N5O7P
  • MW: 347.221
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.3±0.1 g/cm3
  • Boiling Point: 815.5±75.0 °C at 760 mmHg
  • Melting Point: -210ºC (dec.)
  • Flash Point: 447.0±37.1 °C

GNE-6776

GNE-6776 is a selective USP7 inhibitor.

  • CAS Number: 2009273-71-4
  • MF: C20H20N4O2
  • MW: 348.4
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5’-O-(4,4’-Dimethoxytrityl)-2’-beta-C-methyl adenosine

5’-O-(4,4’-Dimethoxytrityl)-2’-beta-C-methyl adenosine 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: 2305415-95-4
  • MF: C32H33N5O6
  • MW: 583.63
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-(6-aminopurin-9-yl)-5-methylidene-oxolane-3,4-diol

4′,5′-Didehydro-5′-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: 20535-04-0
  • MF: C10H11N5O3
  • MW: 249.23
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.91g/cm3
  • Boiling Point: 591.1ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 311.3ºC

SIRT2-IN-10

SIRT2-IN-10 (Compound 12) is a potent SIRT2 inhibitor with an IC50 of 1.3 μM. SIRT2-IN-10 can be used for the research of cancer and neurodegenerative disease[1].

  • CAS Number: 296793-09-4
  • MF: C28H21N5OS
  • MW: 475.56
  • Catalog: Sirtuin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2'-Deoxy-2'-fluoro-D-inosine

2’-Deoxy-2’-fluoroinosine 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: 80049-87-2
  • MF: C10H11FN4O4
  • MW: 270.22
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.01g/cm3
  • Boiling Point: 682.1ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 366.3ºC

Olaparib (AZD2281)

Olaparib (AZD2281;KU0059436) is a potent and oral PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively.

  • CAS Number: 763113-22-0
  • MF: C24H23FN4O3
  • MW: 434.463
  • Catalog: Autophagy
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’-OTBDMS-rU

rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.

  • CAS Number: 118362-03-1
  • MF: C45H61N4O9PSi
  • MW: 861.05
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CA-224

CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity[1].

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

Chetomin

Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule[1].

  • CAS Number: 1403-36-7
  • MF: C31H32N6O6S4
  • MW: 712.882
  • Catalog: Apoptosis
  • Density: 1.8±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 710.9ºC
  • Flash Point: N/A

Novobiocin

Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity[1][2][3][4][6].

  • CAS Number: 303-81-1
  • MF: C31H36N2O11
  • MW: 612.624
  • Catalog: Bacterial
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 848.2±65.0 °C at 760 mmHg
  • Melting Point: 170-172°C (lit.)
  • Flash Point: 466.8±34.3 °C

Boc-Lys(Ac)-AMC

Boc-Lys(Ac)-AMC is a cell-permeable fluorometric HDAC substrate (Ex/Em = 355 nm/460 nm)[1][2].

  • CAS Number: 233691-67-3
  • MF: C23H31N3O6
  • MW: 445.50900
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Palmitic acid-d2-5

Palmitic acid-d2-5 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA 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: 1219805-64-7
  • MF: C16H30D2O2
  • MW: 258.44
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

9H-Purin-6-amine,9-(6-deoxy-b-D-allofuranosyl)-

5’(R)-C-Methyladenosine 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: 3253-81-4
  • MF: C12H17N5O4
  • MW: 295.29
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

9-hydroxystearic acid

9-Hydroxyoctadecanoic acid (9-HSA) is an HDAC1 inhibitor that inhibits ∼66.4% HDAC1 enzymatic activity at 5 μM. 9-Hydroxyoctadecanoic acid shows anticancer activity[1].

  • CAS Number: 3384-24-5
  • MF: C18H36O3
  • MW: 300.48
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N,N'-Dihydroxyoctanediamide

Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) is a competitive and cell-permeable HDAC1 and HDAC3 inhibitor with ID50 values of 0.25 μM and 0.30 μM, respectively[1].Suberoyl bis-hydroxamic acid renders MM cells susceptible to apoptosis and facilitates the mitochondrial apoptotic pathways[2].Suberoyl bis-hydroxamic acid can be used for the study of medullary thyroid carcinoma (MTC)[3].

  • CAS Number: 38937-66-5
  • MF: C8H16N2O4
  • MW: 204.224
  • Catalog: HDAC
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 153-155ºC(lit.)
  • Flash Point: N/A

Samuraciclib

Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib has anti-tumor effects[1][2].

  • CAS Number: 1805833-75-3
  • MF: C22H30N6O
  • MW: 394.51
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

eIF4E-IN-1

eIF4E-IN-1 is a potent inhibitor of eIF4E. eIF4E-IN-1 inhibits immunosuppression components such as immune checkpoint proteins PD-1, PD-L1, LAG3, TIM3, and/or IDO, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease (extracted from patent WO2021003194A1, compound Y)[1].

  • CAS Number: 2573979-31-2
  • MF: C33H28ClF3N6O4S
  • MW: 697.13
  • Catalog: Eukaryotic Initiation Factor (eIF)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ARTD10/PARP10-IN-1

ARTD10/PARP10-IN-1 (compound 23) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 (ARTD1/PARP1) with IC50s of 1.7 μM, 1.6 μM, 0.8 μM, and 4.4 μM, respectively[1].

  • CAS Number: 1708103-76-7
  • MF: C12H12N2O4
  • MW: 248.23
  • Catalog: PARP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BSJ-03-204

BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity[1].

  • CAS Number: 2349356-09-6
  • MF: C43H48N10O8
  • MW: 832.90
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tanshindiol C

Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research[1][2].

  • CAS Number: 97465-71-9
  • MF: C18H16O5
  • MW: 312.317
  • Catalog: Sirtuin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 561.5±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 293.4±30.1 °C

Teniposide

Teniposide is a podophyllotoxin derivative, acts as a topoisomerase II inhibitor, and used as a chemotherapeutic agent.

  • CAS Number: 29767-20-2
  • MF: C32H32O13S
  • MW: 656.654
  • Catalog: Topoisomerase
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 864.3±65.0 °C at 760 mmHg
  • Melting Point: 274 - 277ºC
  • Flash Point: 476.5±34.3 °C

8-NH2-ATP tetrasodium

8-NH2-ATP tetrasodium, an inactive form of ATP, is produced by 8-NH2-Ado. 8-NH2-Ado tetrasodium induces apoptosis-related cleavage of poly (ADP-ribose) polymerase[1][2].

  • CAS Number: 35892-97-8
  • MF: C10H13N6Na4O13P3
  • MW: 610.12
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(E/Z)-BIO-acetoxime

(E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC50=2.4, 4.3, 63 μM)[1].

  • CAS Number: 740841-15-0
  • MF: C18H12BrN3O3
  • MW: 398.21000
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3'-Deoxyuridine-5'-triphosphate

3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM[1].

  • CAS Number: 69199-40-2
  • MF: C9H15N2O14P3
  • MW: 468.14200
  • Catalog: DNA/RNA Synthesis
  • Density: 2.01g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

6-(2-Furanyl)-9-β-D-ribofuranosyl-9H-purine

6-(2-Furanyl)-9-β-D-ribofuranosyl-9H-purine 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: 352025-81-1
  • MF: C14H14N4O5
  • MW: 318.28
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A