DP1 | CAS#N/A | MedKoo

MedKoo Cat#: 535164 | Name: DP1

Description:

WARNING: This product is for research use only, not for human or veterinary use.

DP1 is a novel potent PROTAC, hijacking the E3 ligase complex CRL4-DCAF15 and inducing cellular degradation of BRD4.

Chemical Structure

DP1

CAS#N/A

Theoretical Analysis

MedKoo Cat#: 535164

Name: DP1

CAS#: N/A

Chemical Formula: C42H42ClN9O6S2

Exact Mass: 867.2388

Molecular Weight: 868.43

Elemental Analysis: C, 58.09; H, 4.88; Cl, 4.08; N, 14.52; O, 11.05; S, 7.38

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

Synonym

DP1; DP-1; DP 1

IUPAC/Chemical Name

(S)-N-(2-(2-(2-(2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamido)ethoxy)ethoxy)ethyl)-3-(N-(3-cyano-4-methyl-1H-indol-7-yl)sulfamoyl)benzamide

InChi Key

AXAFSTIEKGDKLM-UMSFTDKQSA-N

InChi Code

InChI=1S/C42H42ClN9O6S2/c1-24-8-13-33(39-36(24)30(22-44)23-47-39)51-60(55,56)32-7-5-6-29(20-32)41(54)46-15-17-58-19-18-57-16-14-45-35(53)21-34-40-50-49-27(4)52(40)42-37(25(2)26(3)59-42)38(48-34)28-9-11-31(43)12-10-28/h5-13,20,23,34,47,51H,14-19,21H2,1-4H3,(H,45,53)(H,46,54)/t34-/m0/s1

SMILES Code

O=C(NCCOCCOCCNC(C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1)=O)C5=CC=CC(S(=O)(NC6=CC=C(C)C7=C6NC=C7C#N)=O)=C5

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 868.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Vijay R, Fehr AR, Janowski AM, Athmer J, Wheeler DL, Grunewald M, Sompallae R, Kurup SP, Meyerholz DK, Sutterwala FS, Narumiya S, Perlman S. Virus-induced inflammasome activation is suppressed by prostaglandin D2/DP1 signaling. Proc Natl Acad Sci U S A. 2017 Jul 3;114(27):E5444-E5453. doi: 10.1073/pnas.1704099114. Epub 2017 Jun 19. PMID: 28630327; PMCID: PMC5502630. 2: Binda C, Génier S, Degrandmaison J, Picard S, Fréchette L, Jean S, Marsault E, Parent JL. L-type prostaglandin D synthase regulates the trafficking of the PGD2 DP1 receptor by interacting with the GTPase Rab4. J Biol Chem. 2019 Nov 8;294(45):16865-16883. doi: 10.1074/jbc.RA119.008233. Epub 2019 Oct 1. PMID: 31575663; PMCID: PMC6851311. 3: Kumar S, Palaia T, Hall C, Ragolia L. DP1 receptor agonist, BW245C inhibits diet-induced obesity in ApoE-/- mice. Obes Res Clin Pract. 2018 Mar- Apr;12(2):229-241. doi: 10.1016/j.orcp.2017.05.003. Epub 2017 Jun 8. PMID: 28602634. 4: Peinhaupt M, Roula D, Theiler A, Sedej M, Schicho R, Marsche G, Sturm EM, Sabroe I, Rothenberg ME, Heinemann A. DP1 receptor signaling prevents the onset of intrinsic apoptosis in eosinophils and functions as a transcriptional modulator. J Leukoc Biol. 2018 Jul;104(1):159-171. doi: 10.1002/JLB.3MA1017-404R. Epub 2018 Apr 1. PMID: 29607536; PMCID: PMC6032830. 5: Kong D, Wan Q, Li J, Zuo S, Liu G, Liu Q, Wang C, Bai P, Duan SZ, Zhou B, Gounari F, Lyu A, Lazarus M, Breyer RM, Yu Y. DP1 Activation Reverses Age- Related Hypertension Via NEDD4L-Mediated T-Bet Degradation in T Cells. Circulation. 2020 Feb 25;141(8):655-666. doi: 10.1161/CIRCULATIONAHA.119.042532. Epub 2020 Jan 2. PMID: 31893939. 6: He Y, Zuo C, Jia D, Bai P, Kong D, Chen D, Liu G, Li J, Wang Y, Chen G, Yan S, Xiao B, Zhang J, Piao L, Li Y, Deng Y, Li B, Roux PP, Andreasson KI, Breyer RM, Su Y, Wang J, Lyu A, Shen Y, Yu Y. Loss of DP1 Aggravates Vascular Remodeling in Pulmonary Arterial Hypertension via mTORC1 Signaling. Am J Respir Crit Care Med. 2020 May 15;201(10):1263-1276. doi: 10.1164/rccm.201911-2137OC. PMID: 31917615; PMCID: PMC7233340. 7: Nir Y, Tononi G. Dreaming and the brain: from phenomenology to neurophysiology. Trends Cogn Sci. 2010 Feb;14(2):88-100. doi: 10.1016/j.tics.2009.12.001. Epub 2010 Jan 14. PMID: 20079677; PMCID: PMC2814941. 8: Takashima N, Ishino S, Oki K, Takafuji M, Yamagami T, Matsuo R, Mayanagi K, Ishino Y. Elucidating functions of DP1 and DP2 subunits from the Thermococcus kodakarensis family D DNA polymerase. Extremophiles. 2019 Jan;23(1):161-172. doi: 10.1007/s00792-018-1070-3. Epub 2018 Nov 30. PMID: 30506100. 9: Doré S, Shafique Ahmad A. Cytoprotective Role of Prostaglandin D2 DP1 Receptor against Neuronal Injury Following Acute Excitotoxicity and Cerebral Ischemia. In: Kobeissy FH, editor. Brain Neurotrauma: Molecular, Neuropsychological, and Rehabilitation Aspects. Boca Raton (FL): CRC Press/Taylor & Francis; 2015. Chapter 10. PMID: 26269890. 10: Brown EN, Lydic R, Schiff ND. General anesthesia, sleep, and coma. N Engl J Med. 2010 Dec 30;363(27):2638-50. doi: 10.1056/NEJMra0808281. PMID: 21190458; PMCID: PMC3162622. 11: Datta A, Nag A, Raychaudhuri P. Differential regulation of E2F1, DP1, and the E2F1/DP1 complex by ARF. Mol Cell Biol. 2002 Dec;22(24):8398-408. doi: 10.1128/mcb.22.24.8398-8408.2002. PMID: 12446760; PMCID: PMC139864. 12: Kohn MJ, Bronson RT, Harlow E, Dyson NJ, Yamasaki L. Dp1 is required for extra-embryonic development. Development. 2003 Apr;130(7):1295-305. doi: 10.1242/dev.00355. PMID: 12588846. 13: Fenno L, Yizhar O, Deisseroth K. The development and application of optogenetics. Annu Rev Neurosci. 2011;34:389-412. doi: 10.1146/annurev- neuro-061010-113817. PMID: 21692661; PMCID: PMC6699620. 14: Kohn MJ, Leung SW, Criniti V, Agromayor M, Yamasaki L. Dp1 is largely dispensable for embryonic development. Mol Cell Biol. 2004 Aug;24(16):7197-205. doi: 10.1128/MCB.24.16.7197-7205.2004. PMID: 15282318; PMCID: PMC479717. 15: Alkire MT, Hudetz AG, Tononi G. Consciousness and anesthesia. Science. 2008 Nov 7;322(5903):876-80. doi: 10.1126/science.1149213. PMID: 18988836; PMCID: PMC2743249. 16: Ahmad AS. PGD2 DP1 receptor stimulation following stroke ameliorates cerebral blood flow and outcomes. Neuroscience. 2014 Oct 24;279:260-8. doi: 10.1016/j.neuroscience.2014.08.050. Epub 2014 Sep 10. PMID: 25218962. 17: Datta A, Sen J, Hagen J, Korgaonkar CK, Caffrey M, Quelle DE, Hughes DE, Ackerson TJ, Costa RH, Raychaudhuri P. ARF directly binds DP1: interaction with DP1 coincides with the G1 arrest function of ARF. Mol Cell Biol. 2005 Sep;25(18):8024-36. doi: 10.1128/MCB.25.18.8024-8036.2005. PMID: 16135794; PMCID: PMC1234342. 18: Lu S, Zhang X, Chen K, Chen Z, Li Y, Qi Z, Shen Y, Li Z. The small subunit of DNA polymerase D (DP1) associates with GINS-GAN complex of the thermophilic archaea in Thermococcus sp. 4557. Microbiologyopen. 2019 Sep;8(9):e00848. doi: 10.1002/mbo3.848. Epub 2019 May 8. PMID: 31069963; PMCID: PMC6741145. 19: Okuda M, Araki K, Ohtani K, Nishimura Y. The Interaction Mode of the Acidic Region of the Cell Cycle Transcription Factor DP1 with TFIIH. J Mol Biol. 2016 Dec 4;428(24 Pt B):4993-5006. doi: 10.1016/j.jmb.2016.11.001. Epub 2016 Nov 5. PMID: 27825926. 20: Labrecque P, Roy SJ, Fréchette L, Iorio-Morin C, Gallant MA, Parent JL. Inverse agonist and pharmacochaperone properties of MK-0524 on the prostanoid DP1 receptor. PLoS One. 2013 Jun 10;8(6):e65767. doi: 10.1371/journal.pone.0065767. PMID: 23762421; PMCID: PMC3677937.