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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Ac-rC Phosphoramidite-15N

Ac-rC Phosphoramidite-15N is 15N labeled Ac-rC Phosphoramidite (HY-W042357). Ac-rC Phosphoramidite is used for the oligoribonucleotide phosphorodithioate modification (PS2-RNA).

  • CAS Number: 1799795-94-0
  • MF: C47H64N415NO9PSi
  • MW: 903.09
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

7-TFA-ap-7-Deaza-2'-dA

7-TFA-ap-7-Deaza-dA is a modified nucleoside. 7-TFA-ap-7-Deaza-dA can be used in the synthesis of deoxyribonucleic acid or nucleic acid.

  • CAS Number: 178420-75-2
  • MF: C16H16F3N5O4
  • MW: 399.324
  • Catalog: DNA/RNA Synthesis
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: 717.4±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 387.6±32.9 °C

2-(4-Methoxyphenyl)ethanol

4-Methoxyphenethyl alcohol, an aromatic alcohol, is the major component in the anise-like odour produced by A. albispathus Hett. 4-Methoxyphenethyl alcohol can inhibits the protein, RNA and DNA synthesis in Escherichia coli[1].

  • CAS Number: 702-23-8
  • MF: C9H12O2
  • MW: 152.190
  • Catalog: DNA/RNA Synthesis
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 257.5±15.0 °C at 760 mmHg
  • Melting Point: 26-28 °C(lit.)
  • Flash Point: 110.2±14.6 °C

4-thiothymidine

4-Thiothymidine 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: 7236-57-9
  • MF: C10H14N2O4S
  • MW: 258.29
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Centrinone

Centrinone is a selective and reversible inhibitor of polo-like kinase 4 (PlK4) with a Ki of 0.16 nM.

  • CAS Number: 1798871-30-3
  • MF: C26H25F2N7O6S2
  • MW: 633.647
  • Catalog: Polo-like Kinase (PLK)
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 924.2±75.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 512.7±37.1 °C

CDK9-IN-12

CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC50 value of 5.41 nM.

  • CAS Number: 1942843-54-0
  • MF: C21H19ClN4O
  • MW: 378.85
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3'-Azido-3'-deoxy-5-fluorocytidine

3'-Azido-3'-deoxy-5-fluorocytidine (Compound 12) is a cytidine derivative.

  • CAS Number: 2095417-18-6
  • MF: C9H11FN6O4
  • MW: 286.22
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Berberine hydrogen sulphate

Berberine sulfate is a natural alkaline, reduces apoptosis, with potent anti-oxidative and anti-inflammatory effect[1].

  • CAS Number: 633-66-9
  • MF: C20H19NO8S
  • MW: 433.432
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

L-Inosine

L-Inosine is the L-configuration of Inosine (HY-N0092). Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects[1][2].

  • CAS Number: 21138-24-9
  • MF: C10H12N4O5
  • MW: 268.22600
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.08
  • Boiling Point: 732.8ºC at 760 mmHg
  • Melting Point: 218ºC
  • Flash Point: N/A

5-Aminosalicylic acid-13C6

5-Aminosalicylic acid-13C6 is the 13C labeled 5-Aminosalicylic Acid[1]. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[2][3][4].

  • CAS Number: 1189709-96-3
  • MF: C7H7NO3
  • MW: 159.09100
  • Catalog: PAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Palbociclib isethionate

Palbociclib isethionate is a highly selective inhibitor of?CDK4/6?with?IC50s?of 11 nM/16 nM, respectively.?

  • CAS Number: 827022-33-3
  • MF: C26H35N7O6S
  • MW: 573.664
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CUDA

CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively[1]. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease[2].

  • CAS Number: 479413-68-8
  • MF: C19H36N2O3
  • MW: 340.501
  • Catalog: PPAR
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 549.4±19.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 286.1±21.5 °C

3’-O-(2-Methoxyethyl)guanosine

3’-O-(2-Methoxyethyl)guanosine is a guanosine analogue. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].

  • CAS Number: 256224-03-0
  • MF: C13H19N5O6
  • MW: 341.32
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ML 323

ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.

  • CAS Number: 1572414-83-5
  • MF: C23H24N6
  • MW: 384.477
  • Catalog: Deubiquitinase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 515.4±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 265.5±32.9 °C

N2-iso-Butyroyl-3’-deoxy-3’-fluoro guanosine

N2-iso-Butyroyl-3’-deoxy-3’-fluoro 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: 2080404-20-0
  • MF: C14H18FN5O5
  • MW: 355.32
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LX7101

LX7101 is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM.

  • CAS Number: 1192189-69-7
  • MF: C23H29N7O3
  • MW: 451.52100
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2(1H)-Pyridinone,4-hydroxy-1-(2,3,5-tri-O-benzoyl-b-D-ribofuranosyl)-

4-Hydroxy-1-(2,3,5-tri-O-benzoyl-β-D-ribofuranosyl)-2(1H)-pyridinone 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: 23220-74-8
  • MF: C31H25NO9
  • MW: 555.53
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.43g/cm3
  • Boiling Point: 709.4ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 382.8ºC

5’-O-Acetyl-5-acetyloxymethyluridine

5’-O-Acetyl-5-acetyloxymethyluridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].

  • CAS Number: 2305416-11-7
  • MF: C14H18N2O9
  • MW: 358.30
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol

3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol, a SIRT1 activator, exhibits significant stimulation of SIRT1 activity. Anti-tumor activity[1].

  • CAS Number: 97744-95-1
  • MF: C30H52O4
  • MW: 476.732
  • Catalog: Sirtuin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 589.8±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 240.1±24.7 °C

NBI42902

NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases[1].

  • CAS Number: 352290-60-9
  • MF: C27H24F3N3O3
  • MW: 495.49
  • Catalog: PERK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 631.0±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 335.4±34.3 °C

2’,3’,5’-Tri-O-acetyl-5-(trifluoromethyl)uridine

2’,3’,5’-Tri-O-acetyl-5-(trifluoromethyl)uridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].

  • CAS Number: 84500-34-5
  • MF: C16H17F3N2O9
  • MW: 438.31
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

9-(3-Deoxy-3-fluoro-β-D-ribofuranosyl)-6-(pyridine-4-yl)purine

9-(3-Deoxy-3-fluoro-β-D-ribofuranosyl)-6-(pyridine-4-yl)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: 1612191-93-1
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DHODH-IN-8

DHODH-IN-8 (Compound 27) is an inhibitor of human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) with IC50s of 0.13 μM and 47.4 μM, and Kis of 0.016 μM and 5.6 μM, respectively. DHODH-IN-8 has antimalarial activity[1].

  • CAS Number: 1148126-03-7
  • MF: C17H13ClN2O2
  • MW: 312.75
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AT-9283 L-lactate

AT9283 lactic acid is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 lactic acid inhibits growth and survival of multiple solid tumors in vitro and in vivo[1][2].

  • CAS Number: 896466-76-5
  • MF: C22H29N7O5
  • MW: 471.51
  • Catalog: Apoptosis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5'-O-(4,4'-dimethoxytrityl)-inosine

5'-O-DMT-Ri can be used in the synthesis of oligoribonucleotides[1].

  • CAS Number: 119898-59-8
  • MF: C31H30N4O7
  • MW: 570.59200
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2,4-D sodium salt

2,4-D sodium salt (Sodium 2,4-dichlorophenoxyacetate) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D sodium salt acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D sodium salt inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[1].

  • CAS Number: 2702-72-9
  • MF: C8H5Cl2NaO3
  • MW: 243.019
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: 345.6ºC at 760 mmHg
  • Melting Point: 215°C
  • Flash Point: 162.8ºC

RO-3306

Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.

  • CAS Number: 872573-93-8
  • MF: C18H13N3OS2
  • MW: 351.445
  • Catalog: CDK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 569.1±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 298.0±32.9 °C

NCGC00029283

NCGC00029283 is a werner syndrome helicase-nuclease (WRN) helicase inhibitor with IC50s of 2.3 μM, 12.5 μM, and 3.4 μM for WRN, BLM and FANCJ helicase, respectively[1].

  • CAS Number: 714240-31-0
  • MF: C18H12FN3O3
  • MW: 337.305
  • Catalog: DNA/RNA Synthesis
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 576.7±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 302.6±32.9 °C

Dimethylenastron

Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM.

  • CAS Number: 863774-58-7
  • MF: C16H18N2O2S
  • MW: 302.391
  • Catalog: Kinesin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 475.6±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 241.4±31.5 °C

ARTD10/PARP10-IN-2

ARTD10/PARP10-IN-2 (compound 19) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 ARTD1/PARP1 with IC50s of 2.0 μM, and 9.7 μM, respectively[1].

  • CAS Number: 1708103-69-8
  • MF: C12H13N3O3
  • MW: 247.25
  • Catalog: PARP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A