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
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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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2'-Deoxyisocytidine

2’-Deoxyisocytidine 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: 123075-23-0
  • MF: C9H13N3O4
  • MW: 227.22
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3MB-PP1

3MB-PP1, a bulky purine analog, is a Polo-like kinase 1 (Plk1) inhibitor. 3MB-PP1 blocks mitotic progression and cell division arise through target Plk1 in in cells expressing analog-sensitive Plk1 alleles. 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used for the research of hypha formation of Candida albicans and cell division[1][2][3].

  • CAS Number: 956025-83-5
  • MF: C17H21N5
  • MW: 295.38200
  • Catalog: DAPK
  • Density: 1.209g/cm3
  • Boiling Point: 475.471ºC at 760 mmHg
  • Melting Point: 136-138ºC
  • Flash Point: 241.356ºC

4’,5’-Didehydro-5’-deoxy thymidine

4’,5’-Didehydro-5’-deoxy thymidine 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: 28034-72-2
  • MF: C10H12N2O4
  • MW: 224.21
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BNC105

BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.IC50 value: Target:BNC105 exhibited excellent potency against a panel of different cancer cell lines with IC50 <1 nM for DU145, Calu-6, MDA-MB-231 etc. The selectivity observed for BNC105 against activated over quiescent HUVECs was also observed in human aortic arterial endothelial cells (HAAECs). BNC105 also exhibited good potency toward the cisplatin resistant cell line A2780cis.

  • CAS Number: 945771-74-4
  • MF: C20H20O7
  • MW: 372.36900
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CDK9-IN-19

CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML)[1].

  • CAS Number: 2479306-60-8
  • MF: C26H22F2N4O5
  • MW: 508.47
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Nitroso-diethylamine D10

N-Nitrosodiethylamine-d10 is the deuterium labeled N-Nitrosodiethylamine[1]. N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.

  • CAS Number: 1219794-54-3
  • MF: (C2D5)2NNO
  • MW: 112.19661778
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-Azido-3’-deoxy-5-methyl-beta-L-uridine

3’-Azido-3’-deoxy-5-methyl-beta-L-uridine 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: 2095417-10-8
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

9-(2’-O-Acetyl-5’-O-benzoyl-3’-O-methyl-beta-D-ribofuranosyl)-6-chloropurine

9-(2’-O-Acetyl-5’-O-benzoyl-3’-O-methyl-beta-D-ribofuranosyl)-6-chloropurine 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: 2072145-46-9
  • MF: C20H19ClN4O6
  • MW: 446.84
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Prexasertib Mesylate Hydrate

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a potent, selective, ATP competitive CHK1 and CHK2 inhibitor, with a Ki of 0.9 nM for CHK1 and IC50s of <1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2 autophosphorylation (S516). Prexasertib Mesylate Hydrate shows potent anti-tumor activity, significantly abrogates the G2/M checkpoint in p53 deficient HeLa cells with an EC50 of 9 nM[1].

  • CAS Number: 1234015-57-6
  • MF: C19H25N7O6S
  • MW: 479.51
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Curcolonol

Curcolonol is a furan type sesquiterpene. Curcolonol can be isolated from several medical herbs. Curcolonol has inhibitory activity for LIM kinase 1. Curcolonol can be used for the research of breast cancer[1].

  • CAS Number: 217817-09-9
  • MF: C15H20O4
  • MW: 264.317
  • Catalog: LIM Kinase (LIMK)
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 424.8±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 210.7±28.7 °C

Tubulin inhibitor 8

Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM[1].

  • CAS Number: 1309925-39-0
  • MF: C21H14N2O3
  • MW: 342.35
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SF2523

SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

  • CAS Number: 1174428-47-7
  • MF: C19H17NO5S
  • MW: 371.414
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CDK4/6-IN-8

CDK4/6-IN-8 (Compound 7p) is a selective CDK4 and CDK6 inhibitor with IC50 values of 5.01 nM and 3.97 nM, respectively[1].

  • CAS Number: 2649120-22-7
  • MF: C18H18N6O5
  • MW: 398.37
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5'-O-DMT-N4-Bz-2'-F-dC

5'-O-DMT-N4-Bz-2'-F-dC is a nucleoside with protective and modification effects.

  • CAS Number: 146954-77-0
  • MF: C37H34FN3O7
  • MW: 651.691
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LCH-7749944

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis[1].

  • CAS Number: 796888-12-5
  • MF: C20H22N4O2
  • MW: 350.414
  • Catalog: Apoptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 580.0±58.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 304.6±32.3 °C

VERU-111

VERU-111 (ABI-231) is a potent and orally bioavailable α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer[1][2][3].

  • CAS Number: 1332881-26-1
  • MF: C21H19N3O4
  • MW: 377.39
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Adenosine-2-carboxamide

Adenosine-2-carboxamide 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: 70255-72-0
  • MF: C11H14N6O5
  • MW: 310.27
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

L-796449

L-796449 is a potent PPARγ agonist. L-796449 shows neuroprotective. L-796449 has the potential for the research of stroke[1].

  • CAS Number: 194608-80-5
  • MF: C28H27ClO4S
  • MW: 495.03
  • Catalog: PPAR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-carboxymethyluridine

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

  • CAS Number: 20964-06-1
  • MF: C11H14N2O8
  • MW: 302.24
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3-TYP

3-TYP is a selective SIRT3 inhibitor, with an IC50 of 16 nM, more potent over SIRT1 (IC50=88 nM), SIRT2 (IC50=92 nM).

  • CAS Number: 120241-79-4
  • MF: C7H6N4
  • MW: 146.14900
  • Catalog: Sirtuin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Epothilone D

Epothilone D is a potent microtubule stabilizer.

  • CAS Number: 189453-10-9
  • MF: C27H41NO5S
  • MW: 491.68
  • Catalog: Microtubule/Tubulin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 657.7±55.0 °C at 760 mmHg
  • Melting Point: 63-66°C
  • Flash Point: 351.6±31.5 °C

CP-775146

CP-775146 is a selective PPARα agonist that binds strongly to the PPARα ligand. CP-775146 efficiently alleviates obesity-induced liver damage, prevents lipid accumulation by activating the liver fatty acid β-oxidation pathway[1].

  • CAS Number: 702680-17-9
  • MF: C26H33NO4
  • MW: 423.54500
  • Catalog: PPAR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N6-Bz-5’-O-DMTr-2’-O-hexadecanyl adenosine

N6-Bz-5’-O-DMTr-2’-O-hexadecanyl 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: 2382942-34-7
  • MF: C54H67N5O7
  • MW: 898.14
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5'-O-DMT-5-Ethynyl-2'-deoxyuridine 3'-CE phosphoramidite

5'-O-DMT-5-Ethynyl-2'-deoxyuridine 3'-CE phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.

  • CAS Number: 188411-06-5
  • MF: C50H57N6O9P
  • MW: 917.00
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TC11

TC11 is a MCL1 degradator and Caspase-9 and CDK1 activator. TC11 structurally relates to immunomodulatory drugs as phenylphthalimide derivative. TC11 induces apoptotic death caused by degradation of MCL1 during prolonged mitotic arrest[1][2].

  • CAS Number: 100823-03-8
  • MF: C20H22N2O2
  • MW: 322.40100
  • Catalog: Bcl-2 Family
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Chloro-N6,N6-dimethyladenosine

2-Chloro-N6,N6-dimethyladenosine 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: 13406-53-6
  • MF: C11H14ClN5O4
  • MW: 315.71
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2,4-Dichlorophenoxyacetic acid

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

  • CAS Number: 94-75-7
  • MF: C8H6Cl2O3
  • MW: 221.037
  • Catalog: DNA/RNA Synthesis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 345.6±27.0 °C at 760 mmHg
  • Melting Point: 137 °C
  • Flash Point: 162.8±23.7 °C

N6-Methyladenosine N1-oxide

N6-Methyladenosine N1-oxide is an adenosine analogue. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. The popular products in this series are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].

  • CAS Number: 113509-54-9
  • MF: C11H15N5O5
  • MW: 297.27
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HDAC6 degrader-3

HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. HDAC6 degrader-3 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin[1].

  • CAS Number: 2785404-83-1
  • MF: C41H41F4N7O11
  • MW: 883.80
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MST312

MST-312 is a telomerase inhibitor. MST-312 is a chemically modified derivative of green tea epigallocatechin gallate (EGCG). MST-312 can be used for the research of cancer, such as multiple myeloma (MM)[1].

  • CAS Number: 368449-04-1
  • MF: C20H16N2O6
  • MW: 380.35100
  • Catalog: Telomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A