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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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 >
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NF-κB >
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PROTAC >
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VD/VDR
Others >
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WF-536

WF-536 is an orally active inhibitor of Rho-associated coiled-coil-containing protein kinase (ROCK). WF-536 has tumor anti-metastatic activity. WF-536 can be used for the research of cancer[1].

  • CAS Number: 539857-64-2
  • MF: C14H16ClN3O
  • MW: 277.75
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MOCPAC

MOCPAC is an HDAC1 specific substrate[1].

  • CAS Number: 787549-26-2
  • MF: C27H31N3O6
  • MW: 493.55
  • Catalog: HDAC
  • Density: 1.246g/cm3
  • Boiling Point: 804.4ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: N/A

PARP7-probe-1

PARP7-probe-1 is a chemiluminescent labeled PARP7 probe. PARP7-probe-1 is a biotinylated probe binding to the PARP7 active site. PARP7-probe-1 can be used for the research of PARP7 function[1].

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

Triapine

Triapine is a novel inhibitor of the M2 subunit of ribonucleotide reductase (RR), and is a potent radiosensitizer.

  • CAS Number: 143621-35-6
  • MF: C7H9N5S
  • MW: 195.245
  • Catalog: DNA/RNA Synthesis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 436.0±55.0 °C at 760 mmHg
  • Melting Point: 234°C(lit.)
  • Flash Point: 217.5±31.5 °C

MC2590

MC2590 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2590 is a inhibitor of HDAC1-3, −6, −8, and −10 (class I/IIb-selective inhibitor) with ic50 of 0.098 μM, 0.156 μM, 0.039 μM, 0.015 μM, 0.047 μM, 0.071 μM, respectively. MC2590 also inhibits HDAC isoforms HDAC4 (IC50=2.73 μM), HDAC5 (IC50=1.35 μM), HDAC7 (IC50=2.06 μM), HDAC9 (IC50=2.79 μM), HDAC11 (IC50=3.98 μM). MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction[1].

  • CAS Number: 2284460-01-9
  • MF: C20H17N3O3
  • MW: 347.37
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-Methyl-4-thiouridine

5-Methyl-4-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: 49555-43-3
  • MF: C10H14N2O5S
  • MW: 274.29
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

WAY-296817

CK1-IN-3 (compound 51) is a AC1 inhibitor with an IC50s 2.22 µM for CK-1δ[1][2].

  • CAS Number: 349438-74-0
  • MF: C17H16N2O3S
  • MW: 328.39
  • Catalog: Casein Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DNA-PK-IN-1

DNA-PK-IN-1 is a potent inhibitor of DNA-PK. DNA-dependent protein kinase (DNA-PK) is a DNA-PK enzyme complex composed of Ku70/Ku80 heterodimer and DNA-dependent protein kinase catalytic subunit (DNA-PKcs). DNA-PK-IN-1 has the potential for the research of cancer diseases (extracted from patent WO2021136463A1, compound 1)[1].

  • CAS Number: 2663850-40-4
  • MF: C23H26N8O2
  • MW: 446.50
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1-(4-thio-beta-D-ribofuranosyl)uracil

4′-Thiouridine (1-(4-thio-beta-D-ribofuranosyl)uracil) 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: 6741-73-7
  • MF: C9H12N2O5S
  • MW: 260.27
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2′,3′-Dideoxy-3′-fluoro-5-methylcytidine

2′,3′-Dideoxy-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: 115249-95-1
  • MF: C10H14FN3O3
  • MW: 243.23
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 420.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 207.8±31.5 °C

MC-VC-PAB-Cyclohexanediamine-Thailanstatin A

MC-VC-PAB-Cyclohexanediamine-Thailanstatin A is a Spliceostatin (HY-16466) analog, and a drug-linker conjugates for ADC, consisting of ADC Cytotoxin Thailanstatin A (HY-129589) and cleavable ADC linker (MC-vc-PAB). MC-VC-PAB-Cyclohexanediamine-Thailanstatin A can be used for ADC synthesis[1].

  • CAS Number: 1609108-96-4
  • MF: C63H91N9O16
  • MW: 1230.45
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GNE-6640

GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively.

  • CAS Number: 2009273-67-8
  • MF: C20H18N4O
  • MW: 330.38
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TAM470

TAM470 is a novel cytolysin, inhibiting tubulin polymerization and microtubule depolymerization. TAM470 can be used in the synthesis of OMTX705 as payload molecule, OMTX705 is a novel FAP-targeting antibody-drug conjugates (ADCs) with antitumor activity[1].

  • CAS Number: 1802498-63-0
  • MF: C41H67N7O6S
  • MW: 786.08
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2,4(1H,3H)-Pyrimidinedione, 5-bromo-1-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-

5-Bromo-2’-deoxy-2’-fluoro-β-D-arabinouridine 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: 69123-97-3
  • MF: C9H10BrFN2O5
  • MW: 325.09
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rev 2’-O-MOE-G(iBu)-5’-amidite

Rev 2’-O-MOE-G(iBu)-5’-amidite 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: 725223-44-9
  • MF: C47H60N7O10P
  • MW: 913.99
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Oxaliplatin

(rel)-Oxaliplatin is a DNA synthesis inhibitor. (rel)-Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and induces apoptosis. (rel)-Oxaliplatin can be used for cancer research[1][2][3].

  • CAS Number: 63121-00-6
  • MF: C8H14N2O4Pt
  • MW: 397.292
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: 193.6ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 75ºC

CX-5011

CX-5011 is a CK2 inhibitor. CX-5011 also induces Rac1 activation. CX-5011 induces apoptosis and induces cancer cell death[1][2].

  • CAS Number: 1333382-30-1
  • MF: C20H11N4NaO2
  • MW: 362.31700
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’-Deoxy-N6-(4-methoxybenzyl)adenosine

2’-Deoxy-N6-(4-methoxybenzyl)adenosine 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: 157640-47-6
  • MF: C18H21N5O4
  • MW: 371.39
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4-N-benzoylgeMcitabine

N4-Benzoyl-2’-deoxy-2’,2’-diflurocytidine 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: 142816-70-4
  • MF: C16H15F2N3O5
  • MW: 367.30
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Palmitic acid-d5

Palmitic acid-d5 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: 1219802-61-5
  • MF: C16H27D5O2
  • MW: 261.45
  • Catalog: HSP
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 340.6±5.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 154.1±12.5 °C

CDK7-IN-10

CDK7-IN-10 is a CDK7 inhibitor with an IC50 of less than 100 nM, extracted from patent WO2021016388A1, compound I-1. CDK7-IN-10 is useful in inhibiting the activity of a kinase. CDK7-IN-10 has the potential of inhibiting cell growth and inducing cell apoptosis[1].

  • CAS Number: 2588110-62-5
  • MF: C29H35N7O3
  • MW: 529.63
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-Me-dC(Ac) amidite

5-Me-dC(Ac) amidite is used for synthesizing DNA or RNA[1].

  • CAS Number: 1873306-74-1
  • MF: C42H52N5O8P
  • MW: 785.865
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Resveratrol analog 2

Resveratrol analog 2 is an analog of Resveratrol (HY-16561). Resveratrol is a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties[1].

  • CAS Number: 915378-82-4
  • MF: C16H13FO3
  • MW: 272.27
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nitidine chloride

Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway[1][2][3][4][5][6].

  • CAS Number: 13063-04-2
  • MF: C21H18ClNO4
  • MW: 383.825
  • Catalog: Apoptosis
  • Density: 1.35g/cm3
  • Boiling Point: 619ºC at 760 mmHg
  • Melting Point: 281-282ºC
  • Flash Point: 189.4ºC

5-Me-3’-dU-2’-phosphoramidite

5-Me-3’-dU-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: 142103-12-6
  • MF: C40H49N4O8P
  • MW: 744.81
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pentanoic acid

Pentanoic acid, a short-chain fatty acid, is a product of bacterial metabolism and are associated with allergic skin disorders. Pentanoic acid activates ROCK signaling pathway.

  • CAS Number: 109-52-4
  • MF: C5H10O2
  • MW: 102.132
  • Catalog: ROCK
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 185.3±3.0 °C at 760 mmHg
  • Melting Point: −20-−18 °C(lit.)
  • Flash Point: 88.9±0.0 °C

Nesuparib

Nesuparib is a potent inhibitor of PARP. Nesuparib is useful for the research of neuropathic pain, neurodegenerative disease, and cardiovascular disease (extracted from patent WO2016200101A2)[1].

  • CAS Number: 2055357-64-5
  • MF: C23H24N6O
  • MW: 400.48
  • Catalog: PARP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Y-39983 HCl

Y-33075 dihydrochloride is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.

  • CAS Number: 173897-44-4
  • MF: C16H18Cl2N4O
  • MW: 353.24600
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2'-C-Methylguanosine

2'-C-Methylguanosine (2'-C-beta-Methylguanosine) 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: 374750-30-8
  • MF: C11H15N5O5
  • MW: 297.27
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.0±0.1 g/cm3
  • Boiling Point: 733.1±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 397.2±35.7 °C

Adenosine,2'-deoxy-N-(3-methyl-2-butenyl)- (9CI)

N6-Isopentenyl-2’-deoxy adenosine, 2’-deoxy riboprine 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: 25775-85-3
  • MF: C15H21N5O3
  • MW: 319.36
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.46g/cm3
  • Boiling Point: 609.7ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 322.5ºC